Cravatt Reagent

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

Cravatt Reagent 是一种有效的选择性 MAGL 抑制剂。 Cravatt Reagent 抑制 MAGL (IC50 = 9.1 nM)。 MJN110 在小鼠神经病理性疼痛模型中产生阿片类药物的抑制作用。

Cravatt Reagent is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

MJN110 (0.01-1000 nM; 4 hours) has the primary serine hydrolase target, hMAGL, with an IC50 of ~1 nM and 10- and 100-fold selectivity windows over ABHD6 and LYPLA1/2, respectively. Western Blot Analysis Cell Line:Human-derived PC3 cells Concentration:0.01, 0.1, 1, 10, 100, 1000 nM Incubation Time:4 hours Result:HMAGL acted as the primary serine hydrolase target with an IC50 of ~1 nM.

MJN110 (i.p.; 0.0818 mg/kg; twice daily for 5.5 days) reverses chronic constriction injury (CCI)-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner. The respective ED50 value (95% confidence limits) is 0.430 (0.233-0.793) mg/kg. Animal Model:Male C57BL/6J mice ranged from 18 to 35 g Dosage:0.0818 mg/kg Administration:I.p.; twice daily for 5.5 days Result:Reversed CCI-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner.

MJN110

Metabolic Enzyme/Protease

Lipase

MAGL

——

——

1438416-21-7

462.3

C22H21Cl2N3O4?

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (540.74 mM)

Clc1ccc(cc1)C(N1CCN(CC1)C(=O)ON1C(=O)CCC1=O)c1ccc(Cl)cc1

4-[bis(4-chlorophenyl)methyl]-1-piperazinecarboxylic acid 25-dioxo-1-pyrrolidinyl ester

(-20℃)

With Ice Pack

≥ 2 years