URB597

Catalog No.S2631

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

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URB597 Chemical Structure

URB597 Chemical Structure
Molecular Weight: 338.4

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

URB597 is available in the following compound libraries:

Product Information

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  • URB597 Mechanism

Product Description

Biological Activity

Description URB597 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]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

Pharmacology Membrane fractions are prepared from brain homogenates, and FAAH activity is assayed using [3H]anandamide (anandamide[ethanolamine-3H], 60 Ci/mmol) as a substrate. Rat brain membranes (50 μg protein) are incubated for 30 min at 37 °C in buffer containing [3H]anandamide and varying concentrations of URB597. At the end of the incubation period, we stopp the reactions with a mixture of chloroform/methanol and measured [3H]ethanolamine in the aqueous phase by liquid scintillation counting.

Animal Study:

[5]

Animal Models Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice
Formulation sterile 0.9% sodium chloride solution
Dosages 0.3 mg/kg
Administration Inject subcutaneously in a single dose 2 hours or 16 hours before killing

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Mor M, et al. J Med Chem, 2004, 47(21), 4998-5008.

[2] Piomelli D, et al. CNS Drug Rev, 2006, 12(1), 21-38.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00916201 Not yet recruiting Schizophrenia Central Institute of Mental Health, Mannheim|Max-Planck I  ...more Central Institute of Mental Health, Mannheim|Max-Planck Institute for Metabolism Research December 2015 Phase 1

Chemical Information

Download URB597 SDF
Molecular Weight (MW) 338.4
Formula

C20H22N2O3

CAS No. 546141-08-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms KDS-4103
Solubility (25°C) * In vitro DMSO 68 mg/mL (200.94 mM)
Ethanol 5 mg/mL (14.77 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Carbamic acid, N-cyclohexyl-, 3'-(aminocarbonyl)[1,1'-biphenyl]-3-yl ester

Tech Support

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