Cravatt Reagent
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- CAS-Nr.
- 1438416-21-7
- Englisch Name:
- Cravatt Reagent
- Synonyma:
- KT195;KT109;HT-01;KT172;MJN110;Cravatt Reagent;MJN110 >=98% (HPLC);BEADRWVIFHOSGN-UHFFFAOYSA-N;MAGL,MJN 110,Inhibitor,Monoacylglycerol lipase,MJN110,MJN-110,inhibit;2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate
- CBNumber:
- CB02750604
- Summenformel:
- C22H21Cl2N3O4
- Molgewicht:
- 462.33
- MOL-Datei:
- 1438416-21-7.mol
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Cravatt Reagent Eigenschaften
- Siedepunkt:
- 561.5±60.0 °C(Predicted)
- Dichte
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- room temp
- L?slichkeit
- DMSO: soluble20mg/mL, clear
- pka
- 5.07±0.10(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
Bildanzeige (GHS) |
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Alarmwort |
Warnung |
Gefahrenhinweise |
Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
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Sicherheit |
P264 |
Nach Gebrauch gründlich waschen. |
P264 |
Nach Gebrauch gründlich waschen. |
P270 |
Bei Gebrauch nicht essen, trinken oder rauchen. |
P301+P312 |
BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
P330 |
Mund ausspülen. |
P501 |
Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen. |
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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.
Global( 43)Lieferanten
- 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