An O-hexafluoroisopropyl carbamate analog of JZL 184 that potently and selectively inhibits MAGL (IC50s = 15

KML29 – 50 mg

Brand:
Cayman
CAS:
1380424-42-9
Storage:
-20
UN-No:
Non-Hazardous - /

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 (Item No. 13158) that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).{20923} At 5-20 mg/kg, KML29 dose-dependently blocks mouse brain MAGL activity in vivo, without any measurable effect on FAAH activity.{20923} As a second generation MAGL inhibitor, KML29 supersedes the low-level cross reactivity that JZL 184 displays for FAAH yet still maintains comparable potency to its parent compound.  

 

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SKU: 11777 - 50 mg Category:

Description

An O-hexafluoroisopropyl carbamate analog of JZL 184 that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM

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

Synonyms: 

Molecular weight: 549.4

CAS: 1380424-42-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Drugs of Abuse||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids||Research Area|Neuroscience|Pain Research

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