Potent, selective inhibitor of monoacylglycerol lipase
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Pristimerin

Item No. 13621

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-hydroxy-9β,13α-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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 3 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

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    25 mg

    $454

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    50 mg

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    Product Description

    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).1 Its actions are rapid, reversible, and noncompetitive.1 Pristimerin (1 µM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells.1 Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. King, A.R., Dotsey, E.Y., Lodola, A., et al. Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem. Biol. 16(10), 1045-1052 (2009).