化合物URB597 T6714
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Product IntroductionBioactivity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 FA
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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
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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