URB597 546141-08-6

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Molecular Weight:

338.4 URB597 is a potent, Orally Bioavailable FAAH Inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1.






Biological Activity


URB597 binds in the hydrophobic pocket and catalytic core of FAAH that
connects the active site residues to the membrane surface of FAAH. URB597 inhibits FAAH activity in human liver microsomes with IC50 of 3 nM. 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.


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.


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. 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.


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. URB597 could reverse most depressive-like symptoms induced by adolescent THC exposure in femal rats.

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Product Categories : Metabolism > FAAH Inhibitor