Comparison

URB597 European Partner

Item no. S2631-25
Manufacturer Selleckchem
CASRN 546141-08-6
Amount 25 mg
Quantity options 100 mg 1 g 10 g 10 mM/1 ml 25 mg 5 mg 500 mg 5 g
Category
Type Inhibitors
Specific against other
Smiles C1CCC(CC1)NC(=O)OC2=CC=CC(=C2)C3=CC(=CC=C3)C(=O)N
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias KDS-4103
Similar products URB597
Available
Storage Conditions
2 years -80 in solvent
Molecular Weight
338, 4
Administration
Inject subcutaneously in a single dose 2 hours or 16 hours before killing
Animal Models
Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice
Dosages
0.3 mg/kg
Formulation
sterile 0.9% sodium chloride solution
IC50
4.6 nM [1], 4.6 nM [1], 4.6 nM [1], 4.6 nM [1], 4.6 nM [1], 4.6 nM [1]
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]
Kinase Assay
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 ug 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.
Solubility (25C)
DMSO 68 mg/mL, Water <1 mg/mL, Ethanol 5 mg/mL
Information
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.
Chemical Name
Carbamic acid, N-cyclohexyl-, 3'-(aminocarbonyl)[1, 1'-biphenyl]-3-yl ester

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 25 mg
Available: In stock
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