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22

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40045	Sivopixant S-600918,Sivopixant	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	Sivopixant (S-600918) 是P2X3受体选择性拮抗剂 (P2X3IC50=4.2 nM; P2X2/3IC50=1100 nM)。Sivopixant 可用于缓解疼痛的研究。
T7748	Dermorphin TFA 皮啡肽三氟乙酸盐	Others; Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others
	Dermorphin TFA 是在两栖类皮肤中发现的天然七肽，是 μ-阿片受体激动剂，可用于抑制神经痛。
T15781	LP-935509	Serine/threonin kinase; AAK1 (AP2 associated kinase 1)	Cell Cycle/Checkpoint; Metabolism; Neuroscience
	LP-935509 是一种选择性的、具有脑渗透的、小分子的衔接蛋白-2 相关激酶1 (AAK1) ATP 竞争性抑制剂，其 IC50=3.3 nM，Ki=0.9 nM。它是一种 BIKE 的有效抑制剂 (IC50=14 nM) 和中度的 GAK 抑制剂 (IC50=320 nM)。它能够逆转 SNL 手术后的疼痛。
T7404	Dermorphin 皮啡肽	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Dermorphin 是在两栖类皮肤中发现的天然七肽，是 μ-阿片受体激动剂，可用于抑制神经痛。
T2264	AM281 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺	Cannabinoid Receptor	GPCR/G Protein
	AM281 是选择性CB1受体拮抗剂，IC50=9.91 nM。它抑制 CB2 受体，IC50=13000 nM。
T9543	Syk Inhibitor II hydrochloride	Others	Others
	Syk Inhibitor II hydrochloride 信号传导的影响在狼疮中可能很突出。
T39026	Ni(II) protoporphyrin IX
	Ni(II) protoporphyrin IX is a metalloporphyrin compound characterized by its limited propensity for axial ligation and its distortion upon binding to ferrochelatase.
T24690	Pyrromecaine HCl Bumecaine hydrochloride,Pyrromecaine
	Pyrromecaine is a local anesthetic used for surface anesthesia. Pyromecaine has a wide spectrum of antiarrhythmic action, exerts a favorable effect on the contractility of the left ventricle, and on the myocardial blood flow following the ligation of the
T38607	Etoposide phosphate disodium BMY-40481 disodium,Etoposide phosphate disodium
	Etoposide phosphate disodium (BMY-40481 disodium), a phosphate ester prodrug of etoposide, functions as a potent chemotherapeutic agent by selectively inhibiting topoisomerase II, hindering the re-ligation of DNA strands. It is regarded as the active equivalent of etoposide, effectively inducing cell cycle arrest, apoptosis, and autophagy in cancer cells.
T83213	AC-099
	AC-099 hydrochloride（化合物 3）作为NPFF2R的选择性全激动剂（EC50=1189 nM）和NPFF1R的部分激动剂（EC50=2370 nM），可降低大鼠脊神经结扎引起的痛觉超敏。
T37845	Taurocholic Acid 3-sulfate (sodium salt)
	Taurocholic acid 3-sulfate (TCA3S) is a metabolite of the conjugated bile acid taurocholic acid .1Plasma levels of TCA3S are elevated in wild-type andSortilin 1(Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated inSort1knockout mice at 24 hours post-BDL.2 1.Lefebvre, P., Cariou, B., Lien, F., et al.Role of bile acids and bile acid receptors in metabolic regulationPhysiol. Rev.89(1)147-191(2009) 2.Li, J., Woolbright, B.L., Zhao, W., et al.Sortilin 1 loss-o...
T70340	JHU-58
	JHU-58 is a novel dipeptide MrgC agonist. JHU-58 inhibited both mechanical and heat hypersensitivity in rats after an L5 spinal nerve ligation (SNL). JHU58 attenuated the evoked excitatory postsynaptic currents in substantia gelatinosa (SG) neurons in wild-type mice, but not in Mrg knockout mice, after peripheral nerve injury.
T79924	T4 RNA ligase	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	T4 RNA ligase为一RNA连接酶，催化单链DNA分子的连接作用。该酶在酶促低核糖核苷酸合成及RNA 3'端标记过程中应用。
T78632	Z-LLY-FMK Calpain Inhibitor IV	Proteasome	Proteases/Proteasome; Ubiquitination
	Z-LLY-FMK (Calpain Inhibitor IV) 为一种钙蛋白酶抑制剂，涉及调控多个细胞系统的凋亡过程。该化合物能够抑制胆总管结扎所引起的肠细胞凋亡(apoptosis)。
T37140	5'-O-DMT-rI
	5’-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1]. [1]. Kadokura M. Synthesis of 4-thiouridine, 6-thioinosine, and 6-thioguanosine 3’,5’-O-bisphosphates as donor molecules for RNA ligation and their application to the synthesis of photoactivatable TMG-capped U1 snRNA fragments. J Org Chem. 2000 Aug 25;65(17):5104-13.
T35461	δ14-Triamcinolone acetonide
	δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a ...
T78803	SIRT5 inhibitor 7	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT5 inhibitor7 (compound 58) 是一种底物竞争性且选择性的SIRT5抑制剂，展现出抗炎活性。它在调节蛋白质琥珀酰化和抑制促炎细胞因子释放方面具有潜在的肾功能保护效果。此外，在LPS和CLP诱导的脓毒症相关急性肾损伤小鼠模型中，SIRT5 inhibitor7已证实具备体内有效性。
T69686	BMS-986318
	BMS-986318 是一种有效的非胆汁酸FXR 激动剂，在FXRGal4 和 SRC-1 募集试验中的EC50分别为 53 和 350 nM。 BMS-986318 具有合适的 ADME 特性，并在肝胆汁淤积和纤维化的小鼠胆管结扎模型中具有效果。BMS-986318 可用于非酒精性脂肪性肝炎 (NASH)的研究。
T83866	LCC-12 formate
	LCC-12是一种铜(II)螯合剂，为二甲双胍的衍生物。作为单体，它能结合铜(II)并在20 µM的浓度下减少氢过氧化物依赖的NADH向NAD+的氧化。在10 µM的浓度下，LCC-12降低一次性人类细胞因子激活的单核衍生的巨噬细胞(MDMs)中IL-1β、IL-2、IL-6、IL-8和TNF-α的细胞因子水平，以及JAK2、STAT2和IL-1受体相关激酶4(IRAK4)的水平。此外，同样浓度的LCC-12减少了细胞因子激活的MDMs中CD80+和CD86+的数量。每日0.3 mg/kg的剂量可提高LPS或盲肠结扎穿孔模型小鼠的存活率。
T83685	UFP101 TFA
	UFP101是一种合成肽类物质，作为nociceptin受体的拮抗剂（Ki为0.06 nM，测试于表达人类受体的CHO细胞中）。它对nociceptin受体的选择性高于κ-opioid受体（Ki为204 nM，测试于表达大鼠受体的CHO细胞中）。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS（EC50为1.86 nM）。通过脑室内给药，UFP101（10 nmol/每只动物）能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中，UFP101（0.003、0.03及0.3 mg/kg）能提高生存率。
T83769	TC 14012 hydrochloride H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2
	TC 14012是一种化学肽模拟的拮抗剂，针对趋化因子(C-X-C motif)受体4（CXCR4；IC50 = 2.9 nM）和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募（EC50 = 350 nM）。TC 14012可减少HIV在MT-4细胞中的细胞病理效应（EC50 = 0.4 nM），并以CXCR4依赖的方式抑制HIV在体外进入（IC50 = 19.3 nM）。它还能抑制由趋化因子(C-X-C motif)配体12（CXCL12）在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞（HUVECs）中诱导的迁移，当使用浓度范围从10到1,000 nM时。在通过左前降（LAD）冠状动脉结扎诱导的急性心肌梗死小鼠模型中，TC 14012（10 mg/kg）能减少梗死面积。
T38309	LL-37 amide (trifluoroacetate salt)
	LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. ...

化合物

Cat.No: T40045

Synonym: S-600918,Sivopixant

Target: P2X Receptor

Cat.No: T7748

Synonym: 皮啡肽三氟乙酸盐

Target: Others, Opioid Receptor

Cat.No: T15781

Target: Serine/threonin kinase, AAK1 (AP2 associated kinase 1)

Cat.No: T7404

Synonym: 皮啡肽

Target: Opioid Receptor

Cat.No: T2264

Synonym: 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺

Target: Cannabinoid Receptor

Syk Inhibitor II hydrochloride

Cat.No: T9543

Target: Others

Ni(II) protoporphyrin IX

Cat.No: T39026

Pyrromecaine HCl

Cat.No: T24690

Synonym: Bumecaine hydrochloride,Pyrromecaine

Etoposide phosphate disodium

Cat.No: T38607

Synonym: BMY-40481 disodium,Etoposide phosphate disodium

Cat.No: T83213

Taurocholic Acid 3-sulfate (sodium salt)

Cat.No: T37845

Cat.No: T70340

Cat.No: T79924

Target: DNA/RNA Synthesis

Cat.No: T78632

Synonym: Calpain Inhibitor IV

Target: Proteasome

Cat.No: T37140

δ14-Triamcinolone acetonide

Cat.No: T35461

SIRT5 inhibitor 7

Cat.No: T78803

Target: Sirtuin

Cat.No: T69686

Cat.No: T83866

Cat.No: T83685

TC 14012 hydrochloride

Cat.No: T83769

Synonym: H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2

LL-37 amide (trifluoroacetate salt)

Cat.No: T38309

Cat. No.	Product Name	Target	Signaling Pathways
T6S1027	Tussilagone	Others	Others
	Tussilagone 是Tussilago farfara 的主要活性成分，具有抗炎作用。它抑制盲肠结扎和穿刺导致脓毒症的小鼠的炎症反应，提高其生存率。它改善葡聚糖硫酸钠诱导的小鼠结肠炎的炎症反应。
T2973	Astragaloside IV AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV	MMP; ERK; Estrogen/progestogen Receptor; JNK	Endocrinology/Hormones; MAPK; Proteases/Proteasome
	Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷，抑制ERK1/2和JNK 激活，在乳腺癌细胞 MDA-MB-231 中，下调(MMP)-2和(MMP)-9的信号通路。

天然产物

Cat.No: T6S1027

Target: Others

Astragaloside IV

Cat.No: T2973

Synonym: AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV

Target: MMP, ERK, Estrogen/progestogen Receptor, JNK

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