| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
CVT-10216 targets aldehyde dehydrogenase 2 (ALDH2). It acts as a potent, selective, and reversible inhibitor. It has an IC50 of 29 nM for ALDH2 and 1300 nM for ALDH1. By inhibiting ALDH2, it modulates aldehyde metabolism.
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| ln Vitro |
CVT-10216 significantly reduces about 50% of ALDH activity in OCI-AML3 cells even in the presence of recombinant TGF-β1 or BM-MSCs. It sensitizes cells to chemotherapy. It is a selective ALDH2 inhibitor.
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| 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].
CVT-10216 sensitizes cells to chemotherapy in vivo. It has been studied for its potential in cancer research. It modulates aldehyde metabolism through ALDH2 inhibition. |
| Enzyme Assay |
CVT-10216 is evaluated in cell-free enzymatic assays using purified ALDH2 and ALDH1 enzymes. The compound is incubated with the enzyme and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of ALDH2 inhibition.
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| Cell Assay |
CVT-10216 is assessed in cell-based assays using OCI-AML3 cells. Cells are treated with CVT-10216, and ALDH activity is measured using biochemical assays. The compound's ability to sensitize cells to chemotherapy is evaluated by measuring cell viability and apoptosis.
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| Animal Protocol |
CVT-10216 is administered in animal models to evaluate its effects on ALDH2 activity and chemotherapy sensitization. It sensitizes cells to chemotherapy. Efficacy is assessed by measuring tumor growth and ALDH activity.
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| ADME/Pharmacokinetics |
CVT-10216 has a molecular weight of 465.5 and a molecular formula of C24H19NO7S. It has a CAS number of 1005334-57-5. The compound is a solid with a density of 1.5. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CVT-10216. The compound is for research use only and is not intended for human therapeutic use. It is a selective ALDH2 inhibitor.
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| References | |
| Additional Infomation |
CVT-10216 is a novel, highly potent, selective, and reversible inhibitor of ALDH2. It is also known as GS 455534. It is an isoflavone compound. It is not approved for clinical use.
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| Molecular Formula |
C24H19NO7S
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|---|---|
| Molecular Weight |
465.475165605545
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| Exact Mass |
465.088
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| CAS # |
1005334-57-5
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| Related CAS # |
1005334-57-5;
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| PubChem CID |
23661666
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
714.2±70.0 °C at 760 mmHg
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| Flash Point |
385.8±35.7 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.676
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| LogP |
3.55
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
857
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| Defined Atom Stereocenter Count |
0
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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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| HS Tariff Code |
2934.99.9001
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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) |
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| 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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