化合物URB597 T6714

Product Introduction
Bioactivity


英文名: URB-597

描述: URB-597 (FAAH Inhibitor II) 是一种可口服的选择性FAAH 抑制剂。 它抑制大鼠脑膜、体外大鼠神经元和人肝微粒体中的 FAAH 活性，IC50分别为 5、0.5和 3 nM。它具有抗抑郁样作用，可研究缓解疼痛。

体外活性: URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface of FAAH. [1] URB597 inhibits FAAH activity in human liver microsomes with IC50 of 3 nM. [2] URB597 reduces the expression of the LPS-induced enzymes cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS; NOS2) in primary rat microglial cell, with a concomitant reduction in the release of the inflammatory mediators prostaglandin E2 (PGE2) and (NO) nitric oxide. [3] URB597 evokes Ca2+ entry in HEK293-F Cells transiently expressing human or rat TRPA1 gene. URB597 also activates Ca2+ entry in rat DRG neurons natively expressed TRPA1 channels. [4]

体内活性: URB597 inhibits [3H]anandamide hydrolysis in rat brain membranes with a parallel increase in brain anandamide, OEA, and PEA content by inhibition of FAAH. URB597 enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH. [5] When delivered intraperitonealy (0.3 mg/kg) URB597 reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain. [6] URB597 reduces the reduction in body weight gain and sucrose intake induced by the chronic mild stress in rats through inhibition of brain FAAH activity. [7] URB597 could reverse most depressive-like symptoms induced by adolescent THC exposure in femal rats. [8]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 5 mg/mL (14.77 mM)
DMSO : 68 mg/mL (200.94 mM)


关键字: Mitochondrial Autophagy | Mitophagy | bioavailable | Autophagy | inhibit | Fatty acid amide hydrolase | URB 597 | Antidepressant-like | Inhibitor | URB-597 | Analgesic | orally | liver | URB597 | microsomes | KDS4103 | KDS 4103 | FAAH

相关产品: Carbamazepine | AICAR phosphate | P62-mediated mitophagy inducer | Salicylic acid | Torkinib | Sunitinib | Quercetin | Resveratrol | Parthenolide | AICAR

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Mitochondria-Targeted Compound Library | Clinical Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | Anti-Obesity Compound Library | Highly Selective Inhibitor Library | Cuproptosis Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途