| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Email: |
orderCN@merckgroup.com |
| Products Intro: |
Product Name:MJN110
CAS:1438416-21-7
Purity:>=98% (HPLC) Package:25MG Remarks:SML0872-25MG
|
Cravatt Reagent manufacturers
- MJN110
-
- $79.00 / 10mg
-
2026-01-29
- CAS:1438416-21-7
- Min. Order:
- Purity: 99.41%
- Supply Ability: 10g
|
| | Cravatt Reagent Basic information |
| Product Name: | Cravatt Reagent | | Synonyms: | 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 | | CAS: | 1438416-21-7 | | MF: | C22H21Cl2N3O4 | | MW: | 462.33 | | EINECS: | | | Product Categories: | | | Mol File: | 1438416-21-7.mol |  |
| | Cravatt Reagent Chemical Properties |
| Boiling point | 561.5±60.0 °C(Predicted) | | density | 1.47±0.1 g/cm3(Predicted) | | storage temp. | room temp | | solubility | DMSO: soluble20mg/mL, clear | | form | powder | | pka | 5.07±0.10(Predicted) | | color | white to beige | | InChI | 1S/C22H21Cl2N3O4/c23-17-5-1-15(2-6-17)21(16-3-7-18(24)8-4-16)25-11-13-26(14-12-25)22(30)31-27-19(28)9-10-20(27)29/h1-8,21H,9-14H2 | | InChIKey | BEADRWVIFHOSGN-UHFFFAOYSA-N | | SMILES | O=C(ON1C(CCC1=O)=O)N2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=C(Cl)C=C4)CC2 |
| Hazard Codes | Xn,N | | Risk Statements | 22-50/53 | | Safety Statements | 26-60-61 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral |
| | Cravatt Reagent Usage And Synthesis |
| Uses | 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] | | Uses | MJN110 has been used as a monoacylglycerol lipase (MAGL) inhibitor to study its effect on aggressive grooming in rats. It has also been used to inhibit lipid droplet formation. | | 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. | | in vivo | 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[1]. | Animal Model: | Male C57BL/6J mice ranged from 18 to 35 g[1] | | 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.
|
|
| | Cravatt Reagent Preparation Products And Raw materials |
|