Powder: -20°C for 3 years | In solvent: -80°C for 1 year
URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 8,000 | |||
10 mg | 在庫あり | ¥ 13,000 | |||
25 mg | 在庫あり | ¥ 28,000 | |||
50 mg | 在庫あり | ¥ 45,500 | |||
100 mg | 在庫あり | ¥ 75,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 14,000 |
説明 | URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets. |
ターゲット&IC50 | FAAH:4.6 nM |
In vitro | 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] |
In vivo | 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] |
別名 | KDS-4103, FAAH Inhibitor II |
分子量 | 338.4 |
分子式 | C20H22N2O3 |
CAS No. | 546141-08-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 5 mg/mL (14.77 mM)
DMSO: 68 mg/mL (200.94 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
URB-597 546141-08-6 Autophagy Metabolism Neuroscience Mitophagy FAAH Mitochondrial Autophagy bioavailable inhibit Fatty acid amide hydrolase URB 597 KDS-4103 Antidepressant-like Inhibitor Analgesic orally liver FAAH Inhibitor II URB597 microsomes KDS4103 KDS 4103 inhibitor