Home Metabolism FAAH inhibitor URB597 For research use only.

URB597

Synonyms: KDS-4103

URB597 (KDS-4103) is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1.

URB597 Chemical Structure

URB597 Chemical Structure

CAS No. 546141-08-6

Purity & Quality Control

Batch: S263101 DMSO]68 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.73%
99.73

URB597 Related Products

Signaling Pathway

FAAH Signaling Pathways

FAAH Signaling Pathway

Biological Activity

Description URB597 (KDS-4103) is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1.
Targets
FAAH [1]
4.6 nM
In vitro
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
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]
Animal Research Animal Models Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice
Dosages 0.3 mg/kg
Administration Inject subcutaneously in a single dose 2 hours or 16 hours before killing

Chemical Information & Solubility

Molecular Weight 338.4 Formula

C20H22N2O3
CAS No. 546141-08-6 SDF Download URB597 SDF
Smiles C1CCC(CC1)NC(=O)OC2=CC=CC(=C2)C3=CC(=CC=C3)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (200.94 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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