Description
KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.
Product information
CAS Number: 1380424-42-9
Molecular Weight: 549.42
Formula: C24H21F6NO7
Chemical Name: 1,1,1,3,3,3-hexafluoropropan-2-yl 4-[bis(2H-1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate
Smiles: OC(C1CCN(CC1)C(=O)OC(C(F)(F)F)C(F)(F)F)(C1C=CC2OCOC=2C=1)C1C=CC2OCOC=2C=1
InChiKey: SXHQLPHDBLTFPM-UHFFFAOYSA-N
InChi: InChI=1S/C24H21F6NO7/c25-23(26,27)20(24(28,29)30)38-21(32)31-7-5-13(6-8-31)22(33,14-1-3-16-18(9-14)36-11-34-16)15-2-4-17-19(10-15)37-12-35-17/h1-4,9-10,13,20,33H,5-8,11-12H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (91.01 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
KML29 dose-dependently elevates brain 2-AG level up to 10-fold without alteration in brain levels of anandamide, palmitoylethanolamide, and oleoylethanolamide. KML29 is a potent inhibitor of 2-AG hydrolysis, but did not affect AEA hydrolysis at any concentration tested.
In Vivo:
KML29 enhibits antinociceptive activity without cannabimimetic side effects. KML29 (20 mg/kg) has a significant but modest protective effect against LPS-induced fever.
Products are for research use only. Not for human use.
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