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URB-597

Catalog No. T6714   CAS 546141-08-6
Synonyms: URB597, FAAH Inhibitor II, KDS-4103

URB597 is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.

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URB-597, CAS 546141-08-6
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description URB597 is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.
Targets&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]
Synonyms URB597, FAAH Inhibitor II, KDS-4103
Molecular Weight 338.407
Formula C20H22N2O3
CAS No. 546141-08-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

Ethanol: 5 mg/mL (14.77 mM)

DMSO: 68 mg/mL (200.94 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Mor M, et al. J Med Chem, 2004, 47(21), 41998-52008. 2. Piomelli D, et al. CNS Drug Rev, 2006, 12(1), 21-38. 3. Tham CS, et al. FEBS Lett, 2007, 581(16), 2899-2904. 4. Niforatos W, et al. Mol Pharmacol, 2007, 71(5), 1209-1216. 5. Fegley D, et al. J Pharmacol Exp Ther, 2005, 313(1), 352-358.

Related compound libraries

This product is contained In the following compound libraries:
Preclinical Compound Library Autophagy Compound Library Anti-Cancer Metabolism Compound Library Anti-Obesity Compound Library Lipid Metabolism Compound Library Inhibitor Library Ion Channel Inhibitor Library Anti-Metabolism Disease Compound Library Drug Repurposing Compound Library Bioactive Lipid Compound Library

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Keywords

URB-597 546141-08-6 代谢 神经科学 自噬 Autophagy FAAH Mitophagy Mitochondrial Autophagy bioavailable inhibit Fatty acid amide hydrolase KDS4103 FAAH Inhibitor II Antidepressant-like KDS-4103 Inhibitor Analgesic orally liver URB597 microsomes KDS 4103 URB 597 inhibitor