URB597 is a relatively selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 4.6 and 0.5 nM in brain membranes and intact neurons, respectively. FAAH is the primary degradatory enzyme for the endocannabinoid anandamide and, as such, inhibition of FAAH leads to an accumulation of anandamide in the CNS and periphery where it activates cannabinoid receptors. URB597 ?produced measurable antidepressant and analgesic effects by increasing endocannabinoids. URB597 ?shows both anti-nociceptive and anxiolytic effects in vivo but not evokes other symptoms associated with cannabinoid-like compounds. Hence, URB597 may provide a new strategy for the treatment of pain and anxiety.
|Source||Cell Physiol Biochem (2018). Figure 1. URB597|
|Cell Lines||WKY rats|
|Incubation Time||two weeks|
|Results||Interestingly, chronic URB597 administration significantly increased intramyocardial glycogen level in the DOCA-salt rats compared to the hypertensive group alone|
|Animal models||Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice|
|Formulation||sterile 0.9% sodium chloride solution|
|Administration||Inject subcutaneously in a single dose 2 hours or 16 hours before killing|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 60 mg/mL|
|Related FAAH Products|
BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH).
JNJ-42165279 is a potent and selective FAAH inhibitor with IC50s of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively.
FAAH-IN-2 is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.
PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.
JNJ-1661010 is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.
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