Cravatt Reagent Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; ) and arachidonoyl ethanolamide (AEA; ) 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. MJN110 is an N-hydroxysuccinimidyl carbamate that inhibits MAGL (IC50 = 9.1 nM) and to a lesser extent ABHD6 with potent selectivity over FAAH (IC50 > 10 μM) and other brain serine hydrolases. It can inhibit 2-AG hydrolysis (IC50 = 2.1 nM) with no effect on AEA hydrolysis up to 50 μM. At 5 mg/kg, MJN110 has been shown to alleviate mechanical allodynia in a rat model of diabetic neuropathy.[Cayman Chemical]

Biochem/physiol Actions

MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). MJN110 inhibits rat, mouse and human MAGL with IC50 values ranging from < 100 nM in rat to an IC50 of ~1 nM with 10- and 100-fold selectivity over closely related ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG, and LYPLA1/2 in human PC3 cells. MJN110 showed potent anti-hyperalgesic activity in a rat model of diabetic neuropathy, showing a therapeutic potential for treating diabetes chronic pain.

Cravatt Reagent Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Cravatt Reagent Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32080	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
TargetMol Chemicals Inc.		support@targetmol.com	United States	38470	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131957	58
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51456	80
Pharmacodia (Beijing) Co.,Ltd	+86-400-851-9921	sales@pharmacodia.com	China	2317	55
Shanghai EFE Biological Technology Co., Ltd.	021-65675885 18964387627	info@efebio.com	China	9806	58
Lynnchem	86-(0)29-85992781 17792393971	info@lynnchem.com	China	4587	58
Novachemistry	44-20819178-90 02081917890	info@novachemistry.com	United Kingdom	4381	58
Shanghai Yu Ben Biotechnology Co., Ltd.	15502154572	yuben012@sina.com	China	508	58

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• 2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate
• Cravatt Reagent
• MJN110
• (2-Benzylpiperidin-1-yl)(4-(2′-methoxy-[1,1′-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)methanone
• KT172
• HT-01
• N-(5-(3-(5,5-Difluoro-7,9-dimethyl-5H-4l4,5l4-dipyrrolo[1,2-c:2′,1′-f][1,3,2]diazaborinin-3-yl)propanamido)pentyl)-N-phenethyl-4-(4-(trifluoromethoxy)phenyl)-1H-1,2,3-triazole-1-carboxamide
• KT195
• (4-([1,1′-Biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone
• KT109
• BEADRWVIFHOSGN-UHFFFAOYSA-N
• 1-Piperazinecarboxylic acid, 4-[bis(4-chlorophenyl)methyl]-, 2,5-dioxo-1-pyrrolidinyl ester
• MJN110 >=98% (HPLC)
• MAGL,MJN 110,Inhibitor,Monoacylglycerol lipase,MJN110,MJN-110,inhibit
• 1438416-21-7