Pristimerin

Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-arachidonoyl glycerol (2-AG), terminating its capacity to activate cannabinoid receptors. Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC50 = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 µM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).Formal Name: 3-hydroxy-9beta,13alpha-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid, methyl ester. CAS Number: 1258-84-0. Synonyms: Celastrol methyl ester, NSC 99281. Molecular Formula: C30H40O4. Formula Weight: 464.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 3 mg/ml. lambdamax: 203, 419 nm. SMILES: O=C1C(O)=C(C)C2=CC=C([C@](CC[C@]3(C)C4C[C@@](C(OC)=O)(C)CC3)(C)[C@@]4(C)CC5)[C@]5(C)C2=C1. InChi Code: InChI=1S/C30H40O4/c1-18-19-8-9-22-28(4,20(19)16-21(31)24(18)32)13-15-30(6)23-17-27(3,25(33)34-7)11-10-26(23,2)12-14-29(22,30)5/h8-9,16,23,32H,10-15,17H2,1-7H3/t23?,26-,27-,28+,29-,30+/m1/s1. InChi Key: JFACETXYABVHFD-RKHSXEAASA-N.