RHC 80267

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets) . RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC) [1][2][3][4].

Product Specifications

CAS Number

[83654-05-1]

Product Name Alternative

U-57908

UNSPSC

12352211

Hazard Statement

H302, H315, H319, H335

Target

Acyltransferase; COX; DAGL; mAChR; Phospholipase

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/rhc-80267.html

Purity

99.41

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(O/N=C1CCCCC\1)NCCCCCCNC(O/N=C2CCCCC/2)=O

Molecular Formula

C20H34N4O4

Molecular Weight

394.51

Precautions

H302, H315, H319, H335

References & Citations

[1] Sutherland CA, et al. Relative activities of rat and dog platelet phospholipase A2 and diglyceride lipase. Selective inhibition of diglyceride lipase by RHC 80267. J Biol Chem. 1982 Dec 10;257 (23) :14006-10.|[2]Ghisdal P, et al. The diacylglycerol lipase inhibitor RHC-80267 potentiates the relaxation to acetylcholine in rat mesenteric artery by anti-cholinesterase action. Eur J Pharmacol. 2005 Jul 4;517 (1-2) :97-102.|[3]Karpińska O, et al. Activation of CB1 receptors by 2-arachidonoylglycerol attenuates vasoconstriction induced by U46619 and angiotensin II in human and rat pulmonary arteries. Am J Physiol Regul Integr Comp Physiol. 2017 Jun 1;312 (6) :R883-R893.|[4]Oglesby TD, et al. The inhibition of arachidonic acid metabolism in human platelets by RHC 80267, a diacylglycerol lipase inhibitor. Biochim Biophys Acta. 1984 Apr 18;793 (2) :269-77.