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Cat. No. | Product Name | Target | Signaling Pathways |
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T7127 |
DC260126
|
Apoptosis; GPR | Apoptosis; Endocrinology/Hormones; GPCR/G Protein |
DC260126 是一种 GPR40 (FFAR1)拮抗剂,对棕榈酸酯诱导的内质网应激和凋亡有保护作用。它剂量依赖性地抑制亚油酸、油酸、棕榈油酸和月桂酸刺激的 GPR40 介导的 Ca2+升高,IC50分别 6.28、5.96、7.07和4.58 μM。 | |||
T69795 |
Crobenetine
BIII 890 CL,Crobenetine Free Base |
Calcium Channel; Sodium Channel | Membrane transporter/Ion channel; Metabolism |
Crobenetine (BIII 890 CL) Free Base 是一种选择性 NaV 通道阻断剂,能消除VTD诱导的[Ca2+]升高。 | |||
T3543 |
NS-638
NS 638 |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
NS-638 是一种 Ca2+ 通道阻滞剂,可阻断 K+ 刺激的细胞内 Ca2+ 升高,IC50值为3.4 μM。 | |||
T15648 |
KDM5-C70
|
Histone Demethylase | Chromatin/Epigenetic |
KDM5-C70 是 KDM5-C49 的乙酯衍生物,是一种有效的细胞渗透性泛 KDM5 组蛋白去甲基化酶抑制剂。它在骨髓瘤细胞中具有抗增殖作用,可诱导全基因组 H3K4me3 水平升高。 | |||
T28958 |
TG6-129
TG6 129 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
TG6-129 是有效的EP2受体选择性拮抗剂,可降低 butaprost 诱导的 P388D1 巨噬细胞中炎症因子的表达。 | |||
T10595 |
BQ-788
BQ788 |
Endothelin Receptor | GPCR/G Protein |
BQ-788 是一种具有选择性和有效性的 ETB 受体拮抗剂,具有潜在的高血压活性,抑制 ET-1 与 ETB 受体结合,抑制外源性 ET-1 诱导的冠状动脉灌注压升高。 | |||
T21704 |
5-fluoro 203
5F-203,NSC-703786 |
Others | Others |
5-fluoro 203 (NSC-703786) 是一种细胞毒性分子。它可激活芳香烃受体(AhR) 信号传导,诱导 CYP1A1 的转录,从而形成 DNA 加合物以及细胞周期阻滞。它可以提高活性氧水平,并激活 ERK、p38以及JNK。 | |||
T1577 |
Midodrine hydrochloride
Pro-Amatine,盐酸米多君 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Midodrine hydrochloride (Pro-Amatine) 通过去甘氨酸反应转化为其活性代谢物 desglymidodrine。Desglymidodrine 选择性地结合并激活小动脉和静脉血管系统的 α-1-肾上腺素能受体。这会导致平滑肌收缩并导致血压升高。 Desglymidodrine 在血脑屏障中的扩散很差,因此与对中枢神经系统的影响无关。Midodrine hydrochloride 是 midodrine 的盐酸盐形式,是一种直接作用的前药和拟交感神经药,具有抗低血压特性。 | |||
T15017 |
CU-T12-9
|
TLR | Immunology/Inflammation |
CU-T12-9 是特异性 TLR1/2激动剂,可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1/2 异二聚体,可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号,引起下游 TNF-α、IL-10 和 iNOS 增加。 | |||
T41005 |
PA-8
|
PACAP | GPCR/G Protein |
PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂,有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化,但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。 | |||
T70993 |
WO-459
|
||
WO-459 is a novel GPR52 agonist, dose-dependently inducing elevation of intracellular cAMP in HEK293/GPR52 cells. | |||
T14068 |
A-192621
|
Others | Others |
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and it also causes elevation of arterial blood pressure and an elevation | |||
T61137 | VEGFR-2-IN-19 | ||
VEGFR-2-IN-19 (Compound 15b) is a highly efficacious inhibitor of VEGFR2, a receptor involved in angiogenesis. Its mechanism of action involves the induction of cellular apoptosis and elevation of intracellular reactive oxygen species. Due to these properties, VEGFR-2-IN-19 holds promise as an effective anticancer agent [1]. | |||
T23583 |
58-G3
58G3 |
||
58-G3 is an agonist of methuselah (Mth)-specific that acts by inducing dose-dependent calcium elevation and membrane translocation of β-arrestin2. | |||
T69991 | Difenamizole HCl | ||
Difenamizole HCl is the salt form of Difenamizole, a non-steroidal anti-inflammatory drug (NSAID) and analgesic of the pyrazolone group related to metamizole. It has monoaminergic properties, including inhibition of monoamine oxidase, augmentation of pargyline-induced elevation of striatal dopamine levels, inhibition of K+-induced striatal dopamine release, and inhibition of the reuptake of dopamine. | |||
T70865 |
BMY-42393
|
||
BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. B... | |||
T27331 |
Flerobuterol HCl
CRL-40996,CRL40996,CRL 40996,Flerobuterol hydrochloride |
||
Flerobuterol is a β adrenergic receptor agonist potentially for the treatment of major depressive disorder. Flerobuterol enhances serotonergic neurotransmission. Flerobuterol acutely increases 5-HT synthesis, in part, through an elevation of brain Trp ava | |||
T68364 |
GS-9160
|
||
GS-9160 is a novel and potent inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase (IN) that specifically targets the process of strand transfer. It is an authentic inhibitor of HIV-1 integration, since treatment of infected cells results in an elevation of two-long terminal repeat circles and a decrease of integration junctions. | |||
T40750 |
12,14-Dichlorodehydroabietic acid
|
||
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, exhibits potent calcium-activated potassium (BK) channel opening activity. It effectively inhibits GABA-dependent chloride influx in the mammalian brain, functioning as a non-competitive antagonist of GABA A receptors. Moreover, 12,14-Dichlorodehydroabietic acid induces an elevation in cytosolic free calcium levels and promotes the release of neurotransmitters. | |||
T81249 | Ru3 | PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Ru3是一种poly(ADP-ribose)polymerase 1抑制剂,能够通过诱导DNA损伤、抑制DNA修复机制、扰乱细胞周期、降低线粒体膜电位及增加reactive oxygen species水平来诱导MCF-7细胞的apoptosis。 | |||
T68760 |
Luminespib mesylate
|
||
Luminespib, also known as AUY-922, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines. | |||
T77026 | Goflikicept | ||
Goflikicept (RPH 104) 是一种可选择性结合并灭活循环中的 IL-1ß 和 IL-1α 的杂合蛋白。此化合物在研究ST段抬高型心肌梗死(STEMI)方面具有潜力。 | |||
T70763 |
KR-67607
|
||
KR-67607, also known as NTX-101 is novel selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. KR-67607 decreased 4-hydroxynonenal expression and increased antioxidant and mucus secretion in BAC-treated rat eyes. KR-67607 showed its protective effects against ischemia-reperfusion-induced eye injury. KR-67607 effectively reduced cortisol levels in mouse eyes and maintained the trabecular meshwork (TM) structure in the presence of transient ischemic stress. Furthermore, KR-67607 rever... | |||
T63088 |
NOD2 antagonist 1
|
||
NOD2 antagonist 1 (compound 32) 是一种有效的、选择性的 NOD2 拮抗剂 (IC50: 5.23 μM)。NOD2 antagonist 1 在 THP-1 细胞,对 Muramyl dipeptide (MDP) 诱导的 IL-8 分泌表现出抑制作用。NOD2 antagonist 1 在 PBMCs 细胞,可以抑制 MDP 诱导的 IL-6、IL-10 和 TNF-α 的水平升高。 | |||
T27228 |
E-3030 free acid
E-3030,E3030,E 3030 |
||
E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr | |||
T63248 | NTU281 | ||
NTU281 是转谷氨酰胺酶-2 (transglutaminase-2) 的有效抑制剂,能够减少糖尿病大鼠血清肌酐和蛋白尿的升高,并降低肾小球 I 型胶原积累、Hic-5 和α-SMA 表达,以及减少细胞凋亡 (apoptosis),能够用于糖尿病引起的肾小球硬化的研究。 | |||
T73083 |
Nipradolol
KT 210 ; K 351 ; Hypadil,Hypadil,KT 210,K 351 |
||
Nipradolol (KT-210; K-351) 是一种有效的 α-1-肾上腺素能受体的阻滞剂。Nipradolol 还抑制白化兔模型中 Phenylephrine 诱导的眼压升高 (IOP)。Nipradolol 抑制去甲肾上腺素 (NA) 引起的肌肉收缩,对犬冠状动脉也有血管扩张剂活性。 | |||
T65252 | Pepsin | ||
Pepsin is an endopeptidase that breaks down proteins into smaller peptides and amino acids that can be easily absorbed in the small intestine[1]. Pepsin is stable at pH ranges as high as pH 6. Above this pH, pepsin is rapidly irreversibly inactivated and elevation of pH of the reaction mixture to pH 8 results in complete inactivation of pepsin[2]. Pepsin has been posited to be a reliable biological marker of EER. An immunologic pepsin assay of combined sputum and saliva was determined to be 100%... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3273 |
Bifendate
联苯双酯,Bifendatatum |
HBV; Reverse Transcriptase | Microbiology/Virology |
Bifendate (Bifendatatum) 是 Schisandrin C 的合成中间体,在慢性 B 型肝炎的研究中具有抗HBV 功效,用于治疗病毒性肝炎和药物性肝损伤引起的转氨酶升高。 | |||
T19924 |
Rhododendrol
Betuligenol,Frambinol,杜鹃醇 |
Others | Others |
Rhododendrol (Frambinol) 是一种黑色素合成物,防止雄性小鼠高脂饮食引起的体重升高和增加雄性小鼠白色脂肪细胞的脂肪分解。Rhododendrol 可用作美白/美白化妆品抑制剂。 | |||
T21344 |
1-Deoxynojirimycin hydrochloride
Moranoline,去氧野艽霉素盐酸盐,AT2220,Duvoglustat hydrochloride,1-Deoxynojirimycin,DNJ,deoxynojirimycin |
PI3K; Antibacterial; Antibiotic; Glucosidase | Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling |
1-Deoxynojirimycin hydrochloride (Moranoline) 是一种口服有效的 α-葡萄糖苷酶抑制剂,具有降血糖、减肥和抗病毒的作用,可抑制餐后血糖,预防糖尿病。 | |||
T0611 |
Vanillylmandelic acid
4-Hydroxy-3-methoxymandelic acid,3-甲氧基-4-羟基扁桃酸 |
Others | Others |
Vanillylmandelic acid (4-Hydroxy-3-methoxymandelic acid) 是儿茶酚胺、肾上腺素和去甲肾上腺素代谢的最终产物,常用于帮助诊断嗜铬细胞瘤,以及其升高与抑郁症状有关。 | |||
T2S1778 |
DL-Goitrin
DL-甲状腺肿素,板蓝根,Goitrin,(R,S)-告依春 |
Others | Others |
DL-Goitrin 也称为 (R,S)-Goitrin,由 epigoitrin (R-Goitrin) 和告依春 (S-Goitrin) 两种异构体组成,是板蓝根的成分。 | |||
T4713 |
Phosphorylcholine chloride calcium salt tetrahydrate
Phosphocholine chloride calcium salt tet,胆碱磷酸氯化钙四水,CalciuM Phosphorylcholine Tetrahydrate |
Others; Endogenous Metabolite | Metabolism; Others |
Phosphorylcholine chloride calcium salt tetrahydrate (Phosphocholine chloride calcium salt tet) 是内源性代谢产物的一种。 | |||
TN1011 |
Rhodionin
|
P450; AChE | Metabolism; Neuroscience |
Rhodionin 是从红景天的根中分离的特异性非竞争性细胞色素 P450 2D6 抑制剂,IC50=0.761 μM,Ki=0.769 μM。它有 DPPH 自由基清除活性,IC50为 19.49 μM。它抑制乙酰胆碱酯酶,IC50范围为 57.50 至 2.43 μg/mL。 | |||
T2860 |
Vanillyl Alcohol
4-Hydroxy-3-methoxybenzenemethanol,3-Methoxy-4-hydroxybenzyl alcohol,4-Hydroxy-3-methoxybenzyl alcohol,香兰醇,Vanillin alcohol,Vanillic alcohol |
Apoptosis; Others | Apoptosis; Others |
Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) 是一种酚类醇,具有抗血管生成、抗惊厥、抗炎、抗氧化、神经保护和抗伤害活性。它由香兰素衍生而来,在食品和饮料中用作调味剂。 | |||
T4877 |
L-Homocystine
|
Endogenous Metabolite | Metabolism |
L-Homocystine 是一种 L-homocysteine 的氧化物。其中 L-homocysteine 是抗血栓因子、血管舒张损害剂、促炎因子,也是研究心血管疾病发生机制的内质网应激反应的诱导剂。 | |||
T5S1632 |
Barlerin
8-O-乙酰山栀苷甲酯,8-O-Acetylshanzhiside methyl ester,ND01 |
VEGFR; TNF; NF-κB; Akt; Caspase | Angiogenesis; Apoptosis; Cytoskeletal Signaling; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
Barlerin (8-O-Acetylshanzhiside methyl ester) 是一种环孢菌素葡萄糖苷,从中国西藏民间药用植物中分离得到,能够抑制NF-κB 活性。 | |||
T4S2326 |
Cornuside
7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside |
ERK; p38 MAPK; NF-κB; JNK | MAPK; NF-κB |
Cornuside (Comuside) 是从山茱萸的果实中分离出的环烯醚萜苷,可用于炎症疾病的研究和促进血液循环。 它通过下调 MAPK 和 NF-κB 信号通路抑制肥大细胞介导的过敏反应,用于炎性过敏性疾病中的潜能。 | |||
T13752 |
L-(+)-Arabinose
|
Endogenous Metabolite | Metabolism |
L-(+)-Arabinose 能够选择性抑制肠道蔗糖酶,并抑制因蔗糖摄入而导致的血浆葡萄糖提高。 | |||
TN2224 |
Soyasapogenol A
大豆甾醇A,大豆甾醇 A |
TNF | Apoptosis |
Soyasapogenol A shows estrogenic and hepatoprotective activities, it directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α±, which consequently resulted in the prevention of liver damage in the concanavalin A-induced hepatitis model. | |||
TN4317 | Isopedicin | NADPH-oxidase; cAMP; p38 MAPK; PKA; JNK; PDE | GPCR/G Protein; Immunology/Inflammation; MAPK; Metabolism; Tyrosine Kinase/Adaptors |
Isopedicin has anti-inflammatory functions, it inhibits the O(2)(*)(-) production in human neutrophils by an elevation of cellular cAMP and activation of PKA through its inhibition of cAMP-specific PDE. | |||
T27564 |
Hymenidin
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
Hymenidin是一种从冲绳海绵Hymeniacidon sp。中分离出的生物碱,是一种5-羟色胺能受体拮抗剂和电压门控钾通道抑制剂,具有潜在的抗原生动物作用,可选择性结合 FOXO1 DNA ,可降低去极化诱导的细胞钙升高。 | |||
TN2169 |
Saikogenin D
柴胡皂甙元 D,皂苷元 D |
IL Receptor; Calcium Channel; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism |
Saikogenin D possesses a dual effect: an inhibition of A23187-induced PGE2 production without a direct inhibition of cyclooxygenase activity; and an elevation of [Ca2+]i that is attributed to Ca2+ release from intracellular stores. Saikogenin D has immuno | |||
TN4582 |
Moracin T
|
c-Myc; COX | Cell Cycle/Checkpoint; Immunology/Inflammation; Neuroscience |
Moracin treatment can inhibit the double 12-O-tetradecanoylphorbol 13-acetate (TPA) treatment-induced morphological changes reflecting inflammatory response, including leucocyte infiltration, hyperplasia and cell proliferation; moracin treatment furthermo |