GPR35

GPR35 is an orphan G protein-coupled receptor (GPCR) that is highly expressed in the gastrointestinal (GI) tract, predominantly in colon epithelial cells (CEC). Kynurenic acid, a metabolite of L-tryptophan, has been proposed to be the endogenous ligand of GPR3535. Upon kynurenic acid-mediated GPR35 activation, β-arrestin 2 translocates to the cell membrane to mediate GPR35 internalization, resulting in receptor desensitization. Single nucleotide polymorphisms of GPR35 have linked this receptor to inflammatory bowel disease and primary sclerosing cholangitis, suggesting a role in gastrointestinal inflammation. In addition, in conjunction with previous findings that link agonism of GPR35 with significant reduction in nociceptive pain, GPR35 has emerged as a potential effector of regulation of mechanical sensitivity and analgesia of the Ret tyrosine kinase, and as a receptor involved in the transmission of anti-inflammatory effects of aspirin– potentially through affecting leukocyte rolling, adhesion and extravasation.

GPR35 相关产品（9）

货号	产品名	Cas	产品描述
PC11381	CID 2745687	264233-05-8	GPR35拮抗剂,CID-2745687对人GPR35的pIC50值为6.70。CID-2745687是一种GPR35拮抗剂。GPR35是一类特征不明显的G蛋白偶联受体A亚家族（视紫红质样受体）的成员。基于GPCR表达水平的差异性，GPCR可作为各类疾病的潜在治疗靶点，包括糖尿病、心血管疾病、炎症以及疼痛。
PL03426	CID1231538	354126-20-8	CID1231538，苯并噻唑类似物，是一种有效的 GPR35 拮抗剂。GPR35 是一种 G蛋白偶联受体 (GPCR)。
PL01621	Kynurenic acid sodium	2439-02-3	Kynurenic acid sodium 是一种内源性色氨酸代谢物，是针对靶点 NMDA, glutamate, α7 nicotinic acetylcholine receptor 的光谱性拮抗剂。Kynurenic acid sodium 也是 GPR35/CXCR8 的激动剂。
PL01623	ML 145	1164500-72-4	ML 145 是选择性，竞争性的人 GPR35/CXCR8 拮抗剂，IC50/EC50 为 20.1 nM。ML 145 对 GPR35 的选择性比 GPR55 (IC50/EC50=21.7 μM) 高超 1000 倍。 ML 145 对啮齿动物直系同源物的 GPR35 均无明显活性。
PC11382	Pamoic acid disodium salt	6640-22-8	GPR35激动剂,Pamoic acid disodium 是一种有效的 GPR35 激动剂，EC50 值为 79 nM。Pamoic acid disodium 诱导 GPR35 内在化并激活 ERK1/2，EC50 值分别为 22 nM 和 65 nM。Pamoic acid disodium 有效地将 β-arrestin2 募集到 GPR35，并具有抗伤害感受的作用。
PC11027	TC-G 1001	494191-73-0	GPR35激动剂
PC11412	TCS 3035	871085-49-3	GPR35激动剂,TCS3035是GPR35的激动剂，对大鼠和人GPR35同源物显示出显著较高的效力，pEC50值分别为5.13和5.86
PC10992	YE 120	383124-82-1	GPR35激动剂,YE-120 is an agonist of G protein-coupled receptor 35 (GPR35).
PC11093	Zaprinast	37762-06-4	磷酸二酯酶抑制剂和GPR35激动剂,Zaprinast (M&B 22948) 是一种 cGMP 选择性的磷酸二酯酶 (PDE) 抑制剂。Zaprinast 是一种 GPR35 激动剂，对大鼠 GPR35 有很强的激活作用，对人 GPR35 有一定的激活作用。Zaprinast 能通过抗增殖和促凋亡作用减少血管重构。