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| 25mg |
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Purity: ≥98%
CVT-10216, an isoflavone compound, is a novel, highly potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) with IC50s of 29 and 1300 nM for ALDH2 and ALDH1, respectively. CVT-10216 increases acetaldehyde after alcohol gavage and inhibits 2-bottle choice alcohol intake in heavy drinking rodents, including deprivation-induced drinking. Moreover, CVT-10216 also prevents operant self-administration and eliminates cue-induced reinstatement of alcohol seeking even when alcohol is not available (i.e., no acetaldehyde). Alcohol stimulates DA release in the NAc, which is thought to contribute to increased drinking and relapse in alcoholism. CVT-10216 prevents alcohol-induced increases in NAc DA without changing basal levels.
| ln Vivo |
In Fawn-Hooded rats, CVT-10216 (ip; 3.75, 7.5, or 15 mg/kg) increased social interactions in a dose-dependent manner; at 15 mg/kg, social interactions increased by double [1]. Five hours following the third medication withdrawal, the intraperitoneal injection CVT-10216 (3.75 or 15 mg/kg) was assessed. Although CVT-10216 at a dose of 15 mg/kg exhibited an anxiolytic effect in this paradigm, it had no discernible effect on locomotor activity [1].
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| References |
[1]. Overstreet DH, et al. A selective ALDH-2 inhibitor reduces anxiety in rats.Pharmacol Biochem Behav. 2009 Dec;94(2):255-61.
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| Molecular Formula |
C24H19NO7S
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|---|---|
| Molecular Weight |
465.475165605545
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| CAS # |
1005334-57-5
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| Related CAS # |
1005334-57-5;
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| SMILES |
O=C(O)C1=CC=CC(COC2=CC=C3C(C(C4=CC=C(NS(=O)(C)=O)C=C4)=COC3=C2)=O)=C1
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| InChi Key |
YYOOFJZTRCPVFD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H19NO7S/c1-33(29,30)25-18-7-5-16(6-8-18)21-14-32-22-12-19(9-10-20(22)23(21)26)31-13-15-3-2-4-17(11-15)24(27)28/h2-12,14,25H,13H2,1H3,(H,27,28)
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| Chemical Name |
3-(((3-(4-(methylsulfonamido)phenyl)-4-oxo-4H-chromen-7-yl)oxy)methyl)benzoic acid
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| Synonyms |
CVT-10216 CVT 10216 CVT10216.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMF : 25 mg/mL (~53.71 mM)
DMSO : ~20 mg/mL (~42.97 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1483 mL | 10.7416 mL | 21.4832 mL | |
| 5 mM | 0.4297 mL | 2.1483 mL | 4.2966 mL | |
| 10 mM | 0.2148 mL | 1.0742 mL | 2.1483 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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