KML29

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KML29 是一种高选择性且有效的单酰基甘油脂肪酶 (MAGL) 抑制剂。

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