1258-84-0

Synonym(s):
(9b,13a,14b,20a)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26 -trinoroleana-1(10),3,5,7-tertraen-29-oic acid methyl ester;Celastrol methyl ester;Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II;Pristimerin - CAS 1258-84-0 - Calbiochem

CAS NO.：1258-84-0

Empirical Formula: C30H40O4

Molecular Weight: 464.64

MDL number: MFCD01711331

PRODUCT Properties

• Melting point: 219.5°C
• Boiling point: 488.1°C (rough estimate)
• Density: 1.0271 (rough estimate)
• refractive index: 1.4800 (estimate)
• storage temp.: -20°C
• solubility: DMSO: ≥5mg/mL
• form: Red solid
• pka: 8.60±0.70(Predicted)
• color: orange
• InChIKey: JFACETXYABVHFD-VXTIGNJVNA-N
• SMILES: [C@]12(C)CC[C@@]3(C)CC[C@@](C)(C(=O)OC)C[C@@]3([H])[C@]1(C)CC[C@@]1(C)C3=CC(C(O)=C(C)C3=CC=C21)=O |&1:0,4,8,15,17,21,r|

Description and Uses

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).

antineoplastic, antiinflammatory

Safety

• Toxicity: LD50 oral in mouse: 8gm/kg