KML29

Research use only, not for human use.

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor.

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

KML29 dose-dependently elevates brain 2-AG level up to10-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.

KML29 enhibits antinociceptive activity without cannabimimetic side effects.KML29 (20 mg/kg) has a significant but modest protective effectagainst LPS-induced fever. Animal Model:C57Bl/6 mice.Dosage:1-40 mg/kg. Administration:P.O. single dose.Result:Selectively inhibited MAGL in mice.Animal Model:Wistar albino male rats.Dosage:20 mg/kg (+LPS E. coli O111:B4 (250 μg/kg, sc)).Administration:SC.Result:Administration of KML29 simultaneously with LPS E. coli O111:B4 significantly decreased ?T (with 5% type 1 error, 1.7 fold) compared to saline+LPS E. coli O111:B4. Administration of KML29 simultaneously with LPS E. coli O111:B4 resulted in decreased plateau phase of fever compared to LPS E. E. coli O111:B4+saline administration.

KML-29 | KML29 | KML 29

Neuroscience

GluR

MAGL

Neurological Disease

——

1380424-42-9

549.42

C24H21F6NO7

>98% (HPLC)

DMSO : 50 mg/mL. 91.01 mM; H2O : < 0.1 mg/mL

O=C(OC(C(F)(F)F)C(F)(F)F)N1CCC(C(c2ccc3OCOc3c2)(O)c2cc3OCOc3cc2)CC1

1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate

(-20℃)

With Ice Pack

≥ 2 years