Identification | Back Directory | [Name]
KML-29 | [CAS]
1380424-42-9 | [Synonyms]
KML-29 CS-2396 KML29 (KML-29) KML29;KML-29;KML 29 4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester 1-Piperidinecarboxylic acid, 4-[bis(1,3-benzodioxol-5-yl)hydroxymethyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester | [Molecular Formula]
C24H21F6NO7 | [MDL Number]
MFCD22987957 | [MOL File]
1380424-42-9.mol | [Molecular Weight]
549.42 |
Chemical Properties | Back Directory | [Melting point ]
204-206°C | [Boiling point ]
554.8±50.0 °C(Predicted) | [density ]
1.511±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
Chloroform (Slightly, Heated, Sonicated), Methanol (Slightly, Heated) | [form ]
Solid | [pka]
13.32±0.29(Predicted) | [color ]
White to Off-White |
Hazard Information | Back Directory | [Description]
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).1 At 5-20 mg/kg, KML29 dose-dependently blocks mouse brain MAGL activity in vivo, without any measurable effect on FAAH activity.1 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. | [Uses]
KML-29 is an extremely specific monoacylglycerol lipase (MAGL) inhibitor. KML-2 should be useful to distinguish between actions of 2-arachidonoyl glycerol (an endogenous ligand of cannabinoid receptors that is deactivated by MAGL) and anandamide, another endocannabinoid. | [storage]
Store at -20°C |
|
|