1005334-57-5
CVT-10216
CAS: 1005334-57-5
Molecular Formula: C24H19NO7S
1005334-57-5 - Names and Identifiers
1005334-57-5 - Physico-chemical Properties
| Molecular Formula | C24H19NO7S |
| Molar Mass | 465.48 |
| Density | 1.468±0.06 g/cm3(Predicted) |
| Boling Point | 714.2±70.0 °C(Predicted) |
| Solubility | DMF : 25 mg/mL (53.71 mM; Need ultrasonic and warming)DMSO : 20 mg/mL (42.97 mM; Need ultrasonic and warming) |
| pKa | 4.13±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | CVT-10216 is a highly selective reversible aldehyde dehydrogenase 2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has ALDH-1 inhibitory effect with IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol consumption in rats with a preference for alcohol and exhibit an anti-anxiety effect. |
| Target | ALDH-2 |
1005334-57-5 - Reference
| Reference Show more | 1: Bocarsly ME, Hoebel BG, Paredes D, von Loga I, Murray SM, Wang M, Arolfo MP, Yao L, Diamond I, Avena NM. GS 455534 selectively suppresses binge eating of palatable food and attenuates dopamine release in the accumbens of sugar-bingeing rats. Behav Pharmacol. 2014 Apr;25(2):147-57. doi: 10.1097/FBP.0000000000000029. PubMed PMID: 24603339. 2: Rezvani AH, Lawrence AJ, Arolfo MP, Levin ED, Overstreet DH. Novel medication targets for the treatment of alcoholism: preclinical studies. Recent Pat CNS Drug Discov. 2012 Aug;7(2):151-62. Review. PubMed PMID: 22574676. 3: Overstreet DH, Knapp DJ, Breese GR, Diamond I. A selective ALDH-2 inhibitor reduces anxiety in rats. Pharmacol Biochem Behav. 2009 Dec;94(2):255-61. doi: 10.1016/j.pbb.2009.09.004. Epub 2009 Sep 10. PubMed PMID: 19747934; PubMed Central PMCID: PMC2859712. 4: Arolfo MP, Overstreet DH, Yao L, Fan P, Lawrence AJ, Tao G, Keung WM, Vallee BL, Olive MF, Gass JT, Rubin E, Anni H, Hodge CW, Besheer J, Zablocki J, Leung K, Blackburn BK, Lange LG, Diamond I. Suppression of heavy drinking and alcohol seeking by a selective ALDH-2 inhibitor. Alcohol Clin Exp Res. 2009 Nov;33(11):1935-44. doi: 10.1111/j.1530-0277.2009.01031.x. Epub 2009 Aug 10. PubMed PMID: 19673742. |
1005334-57-5 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.148 ml | 10.742 ml | 21.483 ml |
| 5 mM | 0.43 ml | 2.148 ml | 4.297 ml |
| 10 mM | 0.215 ml | 1.074 ml | 2.148 ml |
| 5 mM | 0.043 ml | 0.215 ml | 0.43 ml |
Last Update：2024-01-02 23:10:35
1005334-57-5 - Reference Information
| introduction | 3-[[3-[4-[(methylsulfonyl) amino] phenyl]-4-oxo-4H-benzopyran-7-yl] oxy] methyl] benzoic acid is also called 3-[(3-{4-[(methylsulfonyl) amino] phenyl}-4-oxobenzopyranyl-7-yloxy) methyl] benzoic acid, it is a ALDH-2 inhibitor. Ip injection of ALDH-2 inhibitor 3-[[[3-[4-[(methylsulfonyl) amino] phenyl]-4-oxo-4H-benzopyran-7-yl] oxy] methyl] benzoic acid dose-dependent block the recurrence of cocaine. |
| preparation method | to 3-[(3-{4-[(methanesulfonyl) amino] phenyl}-4-oxobenzopyran-7-yloxy) methyl] propyl -2-enyl benzoate (88.8mg,0.176mmol), tetrakis (triphenylphosphine) palladium (0)(10mg,0.009mmol) was added to the solution of dry tetrahydrofuran (2ml) morpholine (77mg,0.88mmol), and the mixture was stirred at room temperature and argon for 2 hours. The solvent is then removed under reduced pressure, and the residue is dissolved in acetone, mixed with silica gel, the solvent is removed under reduced pressure, and then the silica gel is eluted with dichloromethane/methanol (95/5) containing 1% acetic acid, to provide 3-[[[3-[4-[(methylsulfonyl) amino] phenyl]-4-oxo-4H-benzopyran-7-yl] oxy] methyl] benzoic acid. |
Last Update：2024-04-09 21:54:55
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