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T41003
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KG5
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Raf;
FLT;
PDGFR;
c-Kit |
Angiogenesis;
MAPK;
Tyrosine Kinase/Adaptors |
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KG5 是 PDGFRβ 和 B-Raf 的双重变构抑制剂，对 PDGFRβ 和 PDGFRα 的 Kd 分别为 520 nM 和 300 nM。 KG5 抑制 FLT3、KIT 和 c-Raf，具有抗癌和抗血管生成活性。 |
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T67956
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Litoxetine
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5-HT Receptor |
GPCR/G Protein;
Neuroscience |
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Litoxetine 是一种选择性的5-HT 摄取抑制剂，是具有5-HT3受体拮抗剂。Litoxetine 可作为一种抗抑郁剂，在雪貂身上显示出止吐特性。Litoxetine （1和10毫克/公斤静脉注射）剂量依赖性地减少了反胃和呕吐的次数，延迟了呕吐的发生。Litoxetine 对大脑5HT3受体有亲和力（Ki = 85 nM）。 |
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T22697
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CS 2100
1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid
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S1P Receptor |
GPCR/G Protein |
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CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) 是口服有活性 S1P3-sparingS1P1选择性激动剂，对人 S1P1的EC50值为 4.0 nM，对 HvGR 的ID50值为 0.407 mg/kg。它在大鼠体内具有免疫抑制作用。 |
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T4039
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BIBB 515
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Others |
Others |
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BIBB 515 是口服具有活力的 2,3-氧化角鲨烯环化酶选择性抑制剂，在大鼠和小鼠中的 ED50值分别为 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小时)。它主要利用抑制低密度脂蛋白的产生，从而发挥降脂作用。 |
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T36126
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TMP-153
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Acyl-CoA:cholesterol acyltransferase (ACAT) catalyses the esterification of excess cellular cholesterol with fatty acids and is important for intestinal cholesterol absorption, hepatic lipoprotein secretion, and cholesterol accumulation in vascular tissues. ACAT inhibitors improve plasma lipid profile and ameliorate proteinuria in nephrotic animals. TMP-153 is a quinolyl derivative that inhibits ACAT with IC50 values of 5-10 nM in various animals. At 0.5-1.5 mg/kg, TMP-153 dose-dependently reduc... |
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T37816
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SB 243213
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SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].
SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows... |
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T35666
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PRGL493
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Others |
Others |
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PRGL493为高效、选择性的长链酰基辅酶a合成酶4 (ACSL4) 抑制剂，能在乳腺和前列腺细胞以及动物模型中抑制细胞增殖和肿瘤生长，主要应用于癌症研究。 |
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T36696
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DMBA
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7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase... |
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T36949
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Niaprazine
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5-HT Receptor;
Adrenergic Receptor;
Histamine Receptor |
GPCR/G Protein;
Immunology/Inflammation;
Neuroscience |
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Niaprazine 是有效的组胺 H1 受体拮抗剂，具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。 |
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T35689
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MTP 131 acetate
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Others |
Others |
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MTP 131 acetate 是一种小的线粒体靶向四肽。 |
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T38192
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Unifiram
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Others |
Others |
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Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。 |
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T37190
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L-Allylglycine
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Dehydrogenase;
GABA Receptor |
Membrane transporter/Ion channel;
Metabolism;
Neuroscience |
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L-Allylglycine 是 GABA 合成酶（谷氨酸脱羧酶）的有效抑制剂。 |
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T36520
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COR659
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Cannabinoid Receptor;
GABA Receptor |
GPCR/G Protein;
Membrane transporter/Ion channel;
Neuroscience |
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COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。 |
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T38294
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4-Deoxypyridoxine hydrochloride
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S1P Receptor |
GPCR/G Protein |
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4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。 |
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T24742
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RS-67333
RS67333
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RS-67333 is a 5-HT4R partial agonist. It shows efficacy at 0.3 and 1.0 mg/kg, ip. |
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T61639
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S1P1 agonist 4
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S1P1 agonist 4 在效价（EC50< 0.05 mg/kg）和预测人类半衰期方面都有更好的表现 （t1/2 ～ 5 天）。 |
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T79399
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E2730
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GABA Receptor |
Membrane transporter/Ion channel;
Neuroscience |
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E2730是一种针对γ-氨基丁酸(GABA)转运蛋白1(GAT1)的非竞争性选择性抑制剂，它能口服有效且有抗癫痫的作用。这种化合物能够随着环境中GABA水平的增加而增强其抑制GAT1的活性，从而有选择性地抑制GABA的回收。在实验模型中，E2730 (剂量范围为5-50 mg/kg; 经口给药) 在大鼠杏仁核点燃模型和小鼠的多种癫痫模型中，包括角膜点燃 (5-50 mg/kg)、耐药的6Hz-44mA精神运动癫痫 (5-50 mg/kg)、脆性X综合征 (2.5-300 mg/kg) 及Dravet综合征模型 (10 mg/kg, 20 mg/kg)，展现了显著的体内活性。 |
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T37114
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SB 242084 dihydrochloride
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SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.... |
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T36543
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Prostaglandin B2
PGB2
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Prostaglandin B2 (PGB2) is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 ug/kg). [1] |
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T35513
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13C15-Nivalenol
13C15-Nivalenol
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13C15-Nivalenol is intended for use as an internal standard for the quantification of nivalenol by GC- or LC-MS. Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It is lethal to mice (LD50= 6.9 mg/kg).2Nivalenol (5, 10, and 15 mg/kg) also induces thymic, splenic, and Peyer's patch cell apoptosis in mice.3
1.Yang, Z., Concannon, J., Ng, K.S., et al.Tetrandrine identified in a small molecule screen to activate mesenchymal stem cells for enhanced immunomodulationSci. Rep.63026... |
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T38209
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Hodgkinsine
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Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg/kg.
1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000) |
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T34707
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SST-02
SST 02,SST02
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SST-02 is a potent cationic lipid for siRNA-Lipid Nanoparticles. SST-02 possesses a simple chemical structure and is synthesized just in one step. SST-02 showed an ID50 of 0.02 mg/kg in the factor VII (FVII) model. Rats administered with 3 mg/kg of SST-02 |
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T36811
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uPSEM 817 tartrate
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Selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channel agonist (EC50 values are 0.3 and 0.5 nM, respectively). Suppresses firing of layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices. Increases contralateral rotation in mice expressing PSAM4-GlyR unilaterally in the substantia nigra reticulata (LED 0.1 mg/kg).
Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science 3... |
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T79735
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DHFR-IN-9
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DHFR-IN-9（化合物8A）是一种二氢叶酸还原酶（DHFR）抑制剂，通过干扰细胞内嘌呤和胸苷酸的生物合成而影响细胞生长和增殖。该化合物对抗耐甲氧西林金黄色葡萄球菌（MRSA）ATCC 43300展现出显著的抑制效果（IC50=0.25 μg/mL），并在全身及大腿感染的小鼠模型中显示出抗感染能力（剂量：2.5 mg/kg，5 mg/kg；ip）。此外，DHFR-IN-9在乳腺癌小鼠模型中展示了超过紫杉醇（Y-B0015）的抗癌活性（剂量：2.5 mg/kg；ip；每3天1次）。 |
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T35439
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(E)-5-(2-Bromovinyl)uracil
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(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol/kg, increasing survival time. |
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T36639
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Donecopride (fumarate hydrate)
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Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value... |
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T35517
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4-deoxy Nivalenol-13C15
4-deoxy Nivalenol-13C15
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4-deoxy Nivalenol-13C15is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It binds to eukaryotic ribosomes and inhibits protein synthesis in mice when administered at doses ranging from 5 to 25 mg/kg. 4-deoxy Nivalenol (0.1 and 0.2 mg/kg) induces emesis in pigs and decreases feed consumption in pigs when administered at a dose of 40 ppb in the diet.2It induces leth... |
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T69104
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SAX-187 hydrochloride
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SAX-187 hydrochloride is a potent and selective 5-HT6 receptor agonist. SAX-187 hydrochloride possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (SAX-187 hydrochloride: EC50=6.6 nM, Emax=93%). In the rat frontal cortex, acute administration of SAX-187 hydrochloride (3-30 mg/kg, subcutaneous (s.c.)) significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine. |
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T36296
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BIO5192 hydrate
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BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].
The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days... |
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T36160
|
8-iso Prostaglandin E2
8-iso Prostaglandin E2
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8-iso PGE2 is one of several isoprostanes produced from arachidonic acid during lipid peroxidation. It is a potent renal vasoconstrictor in the rat. 8-iso PGE2 inhibits U-46619 or I-BOP-induced platelet aggregation with IC50 values of 0.5 and 5 μM, respectively. When infused into the renal artery of the rat at a concentration of 4 μg/kg/min, 8-iso PGE2 decreases the GFR and renal plasma flow by 80% without affecting blood pressure. |
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T35783
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Zearalenone-13C18
Zearalenone-13C18
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Zearalenone-13C18is intended for use as an internal standard for the quantification of zearalenone by GC- or LC-MS. Zearalenone is a mycotoxin that has been found inFusariumand has estrogenic activities.1It binds to human estrogen receptor α (ERα) and ERβ (IC50s = 9 and 5.8 nM, respectively).2Zearalenone induces precocious development of mammary tissues in young female pigs and prepucial enlargement in young male pigs.3Zearalenone (1.5-5 mg/kg of diet) induces hyperestrogenism in pigs. It also i... |
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T37791
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A-971432
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A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s ... |
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T36101
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Psychotridine
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Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg/kg.3
1.Beretz, A., Roth-Georger, A., Corre, G., et al.Pol... |
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T37391
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PSEM 308 hydrochloride
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PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene.
Lovett-Barron et al (2012) Regulation of neu... |
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T83887
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SLU-10482
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SLU-10482是一种抗寄生虫化合物，能减少HCT-8细胞中C. parvum寄生虫的数量（EC50 = 0.07 µM）。相较于另一种抗寄生虫化合物SLU-2633，SLU-10482与人类ether-a-go-go (hERG; Kd = 43 µM)的结合能力较弱。在体内，SLU-10482以5和15 mg/kg的剂量，每天两次给药，能减少C. parvum感染小鼠模型中粪便中卵囊的数量。 |
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T64553
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GLP-1(7-37) TFA salt
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The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine into the bloodstream in response to food and stimulate insulin secretion. GLP-1(7-37) produced a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration and an increased rate of glucose infusion in Sprague-Dawley Rats at a dosing rang of 0.5, ... |
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T83670
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F1 TFA
Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide
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F1是一种抗炎肽，由HIV-1 Tat蛋白质转导域与对应于抑制因子NF-κB激酶-相互作用肽（IKIP）46-60残基的15氨基酸肽链接而成。在5 µM浓度下，F1抑制了小鼠腹腔巨噬细胞中LPS诱导的IκB激酶α（IKKα）和IKKβ的磷酸化以及NF-κB（p65）的核内转移。在体内，F1（5 mg/kg）降低了LPS诱导的脓毒症小鼠模型中IL-6、TNF-α和IL-1β的血清水平，并增加了生存率。 |
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T36404
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PRLX-93936
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PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM... |
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T36054
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D13
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D13 is an acylhydrazone antifungal.1 It is active against C. neoformans in vitro (MIC80 = 0.06 μg/ml). D13 (20 mg/kg per day, p.o.) increases survival in mouse models of C. neoformans, C. albicans, or A. fumigatus infection.
|1. Lazzarini, C., Haranahalli, K., Rieger, R., et al. Acylhydrazones as antifungal agents targeting the synthesis of fungal sphingolipids. Antimicrob. Agents Chemother. 62(5), e00156-00118 (2018). |
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T71328
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Theobromine-d6
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Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium.... |
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T83665
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α-Helical CRF (9-41) TFA
α-Helical Corticotropin-Releasing Factor (9-41)
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α-Helical CRF (9-41) 是一种合成的皮质酮释放因子（CRF）拮抗剂。它在0.5至5 µM浓度范围内，能抑制CRF诱导的大鼠前叶垂体细胞释放促肾上腺皮质激素（ACTH）。在体内研究中，α-Helical CRF (9-41) (0.02-0.6 µmol/kg) 能够抑制未经麻醉的完整大鼠体内CRF诱导的ACTH释放，并在0.6 µmol/kg剂量下抑制大鼠应激诱导的ACTH释放。此外，α-Helical CRF (9-41) 在尼古丁诱导的条件性焦虑大鼠模型中增加社交互动时间，并减少小鼠的类似暴饮暴食的乙醇消费。 |
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T36629
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Givinostat
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Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1... |
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T37167
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Reduced Haloperidol
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Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ... |
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T68332
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AKI-001
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AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near s... |
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T28884
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SUN-C5174
SUNC-5174
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SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma |
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T83776
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Dopamine D3 Receptor Agonist 13a
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Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合，相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM，分别)具有更高的亲和力，并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM，分别)结合；然而，它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM，在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上，当剂量为3 mg/kg时，Dopamine D3 受体激动剂13a能减少可卡因自我给药。 |
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T71300
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Pentoxifylline-d6
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Pentoxifylline-d6 is intended for use as an internal standard for the quantification of pentoxifylline by GC- or LC-MS. Pentoxifylline is a hemorrheologic agent. It increases the deformability of washed isolated human erythrocytes when used at a concentration of 100 µM. Pentoxifylline (1, 2, and 3 mM) inhibits ADP-induced platelet aggregation in isolated human whole blood. It inhibits thrombus formation induced by ADP in a hamster cheek pouch model when administered at doses of 5, 10, and 20 mg/... |
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T78810
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BWA-522
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Androgen Receptor |
Endocrinology/Hormones |
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BWA-522是一种口服有效的小分子PROTACs，针对AR-FL和AR-V7显示出显著的降解活性。该化合物通过对Androgen Receptor的AR-NTD进行拮抗，诱发PC细胞的apoptosis。在LNCaP异种移植模型中，BWA-522以每日60 mg/kg的剂量口服给药，实现了76%的肿瘤生长抑制(TGI=76%)。在VCaP和LNCaP细胞系中对AR-V7和AR-FL的降解效率分别达到77.3%(1 μM)和72.0%(5 μM)。 |
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T36108
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YW3-56 (hydrochloride) (technical grade)
YW3-56 (hydrochloride) (technical grade)
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YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg/kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2
1.Wang, Y., Li, P., Wang, S., et al.Anticancer pept... |
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T70960
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Maprotiline-d3 hydrochloride
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Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in r... |
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