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19

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T21874	CID 2745687	GPR	Endocrinology/Hormones; GPCR/G Protein
	CID 2745687 是可逆的、特异性 GPR35竞争性拮抗剂（Ki:12.8 nM）。
T8329	AR 231453	GPR	Endocrinology/Hormones; GPCR/G Protein
	AR 231453 是一种口服具有活性的、特异性的 GPR119激动剂。它能够刺激细胞增殖，改善胰岛 β 细胞的功能。
T10363	Arazine N-Acetyl-S-farnesyl-L-cysteine	Others	Others
	Arazine (N-Acetyl-S-farnesyl-L-cysteine) 可以成为异戊二烯基半胱氨酸甲基转移酶的底物通过与异戊二烯化 G 蛋白或其受体位点竞争。 Arazine 是 G 蛋白和 GPCR 信号传导的细胞渗透性调节剂。
T3433	TUG-891 TUG 891,TUG891	GPR	Endocrinology/Hormones; GPCR/G Protein
	TUG-891 是一种选择性的长链游离脂肪酸受体 4 (FFA4/GPR120) 的激动剂。
T50088	N-phenylthiophene-2-carboximidamide	Others	Others
	N-phenylthiophene-2-carboximidamide 是一种噻吩衍生物，可以作为蛋白酪氨酸激酶（PTKs）的抑制剂和 G 蛋白偶联受体（GPCR）的配体发挥作用。
T10843	CMF019	Apelin receptor	GPCR/G Protein
	CMF019 是一种有效的小分子 Apelin receptor (APJ) 激动剂，具有 G protein 偏向性。 CMF019 在人，大鼠和小鼠中与 APJ 结合的 pKi 值分别为 8.58、8.49 和 8.71。CMF-019 在啮齿动物中的有益于心血管。 Apelin 受体 (APJ) 是由内源性肽 apelin 激活的 G 蛋白偶联受体(GPCR)。
T9146	ms48107 Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-	Others	Others
	MS48107 是 G 蛋白偶联受体 68 (GPR68) 的选择性正变构调节剂，对GPR68的选择性高于密切相关的神经递质转运蛋白，质子 GPCR 和 hERG 离子通道。它可以穿越过小鼠的血脑屏障。
T26962	CBP-307 CBP307
	CBP-307 is a selective second generation S1P1 (a G-protein coupled receptor -GPCR) modulator.
T27428	GP-1681 GP 1681,GP1681
	GP-1681, a G-protein coupled receptor (GPCR) agonist, is used potentially for the treatment of influenza infection.
T73005	PF-07054894
	PF-07054894 是一种有效的 CCR6拮抗剂。 PF-07054894 靶向 G 蛋白偶联受体 (GPCR)。 PF-07054894 可用于炎症性肠病的研究。
T83743	VPM-p15 TFA T1V/F3Phe(4-Me)
	VPM-p15是一种合成多肽激动剂，针对粘附G蛋白偶联受体(GPCR) G2 (ADGRG2)而设计，ADGRG2是一种孤儿GPCR，与男性不育有关。在表达人类ADGRG2的HEK293细胞中，它能诱导cAMP积累（EC50 = 1.41 µM）。
T63340	CCG-273220
	CCG-273220 是 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 共价抑制剂 (IC50: 220 nM)。CCG-273220 可以共价结合GRK5亚家族特异性残基 Cys474 ，而对GRK5的选择性比 GRK2 高。
T81683	Neuromedin S (human)
	Neuromedin S (human) 是包含33个氨基酸的神经肽，作为G 蛋白偶联受体 (GPCR) FM-4/TGR-1的内源性配体，在大脑中被鉴定，并对神经调节素 U (NMU) 受体 2 (NMUR2)调节体重稳态具有调控作用。
T69953	MK-8666 Tris
	MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.
T70468	MK-8666
	MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.
T36578	Boc-Lys(Ac)-AMC
	Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1] G2A/GPR132 belongs to the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. GPR132/G2A is first reported to be a transcriptional target for BCR-ABL tyrosine kinase attenuating B-cell expansion in vitro and arresting cells at G2 during mitosis. It has been involved in autoimmune disease and atherosclerosis. [1]...
T77789	Oleoyl-L-alpha-lysophosphatidic acid sodium salt LPA sodium salt
	Oleoyl-L-alpha-lysophosphatidic acid sodium salt为必需的细胞膜生物合成代谢物，可通过与G蛋白偶联受体（GPCR）（即LPA受体）相互作用来介导信号传导，是LPA1和LPA2受体的内源性激动剂。
T83926	S-Geranylgeranyl-L-glutathione GGG
	S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体（GPCR）P2RY8的配体。该化合物在100 nM浓度下，选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2（S1P2）、GPR55、半胱氨酸白三烯受体1（CysLT1 receptor）以及CysLT2 receptor的内吞作用。在10 nM浓度下，S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子（C-X-C motif）配体12（CXCL12）诱导的迁移。
T36550	CAY10535
	TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for ...

化合物

Cat.No: T21874

Target: GPR

Cat.No: T8329

Target: GPR

Cat.No: T10363

Synonym: N-Acetyl-S-farnesyl-L-cysteine

Target: Others

Cat.No: T3433

Synonym: TUG 891,TUG891

Target: GPR

N-phenylthiophene-2-carboximidamide

Cat.No: T50088

Target: Others

Cat.No: T10843

Target: Apelin receptor

Cat.No: T9146

Synonym: Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-

Target: Others

Cat.No: T26962

Synonym: CBP307

Cat.No: T27428

Synonym: GP 1681,GP1681

Cat.No: T73005

Cat.No: T83743

Synonym: T1V/F3Phe(4-Me)

Cat.No: T63340

Neuromedin S (human)

Cat.No: T81683

Cat.No: T69953

Cat.No: T70468

Boc-Lys(Ac)-AMC

Cat.No: T36578

Oleoyl-L-alpha-lysophosphatidic acid sodium salt

Cat.No: T77789

Synonym: LPA sodium salt

S-Geranylgeranyl-L-glutathione

Cat.No: T83926

Synonym: GGG

Cat.No: T36550

Cat. No.	Product Name	Target	Signaling Pathways
TN5580	Rediocide A
	Rediocide A, an insecticide, can inhibit calcium mobilization in Drosophila G-protein- coupled receptors (GPCR)s other than methuselah, it can induce GPCR desensitization and internalization, and such effects are mediated by the activation of conventional

天然产物

Cat.No: TN5580

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