research use only
Cat.No.S2631
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Other FAAH Inhibitors | Biochanin A PF-3845 JNJ-42165279 PF-04457845 FAAH-IN-2 JZL195 URB937 JNJ-1661010 BIA 10-2474 LY-2183240 |
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In vitro |
DMSO
: 68 mg/mL
(200.94 mM)
Ethanol : 4 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 338.4 | Formula | C20H22N2O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 546141-08-6 | Download SDF | Storage of Stock Solutions |
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| Synonyms | KDS-4103 | Smiles | C1CCC(CC1)NC(=O)OC2=CC=CC(=C2)C3=CC(=CC=C3)C(=O)N | ||
| Targets/IC50/Ki |
FAAH
4.6 nM
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|---|---|
| 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. This compound inhibits FAAH activity in human liver microsomes with IC50 of 3 nM. It 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. This chemical evokes Ca2+ entry in HEK293-F Cells transiently expressing human or rat TRPA1 gene. It also activates Ca2+ entry in rat DRG neurons natively expressed TRPA1 channels.
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| 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. This compound enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH. When delivered intraperitonealy (0.3 mg/kg) it reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain. This chemical reduces the reduction in body weight gain and sucrose intake induced by the chronic mild stress in rats through inhibition of brain FAAH activity. It could reverse most depressive-like symptoms induced by adolescent THC exposure in femal rats.
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References |
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