CVT-10216

CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM.

CVT-10216 Chemical Structure

CVT-10216 Chemical Structure

CAS: 1005334-57-5

Purity & Quality Control

Batch: E035501 DMSO] 93 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.73%
99.73

CVT-10216 Related Products

Choose Selective Dehydrogenase Inhibitors

Biological Activity

Description CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM.
Targets
ALDH-2 [1] ALDH-1 [1]
29 nM 1.3 μM
In vitro
In vitro

CVT-10216 significantly reduces about 50% of aldehyde dehydrogenase (ALDH) activity in OCI-AML3 cells even in the presence of recombinant TGF-β1 or BM-MSCs, sensitizing cells to chemotherapy.[2]

Cell Research Cell lines OCI-AML3 cells
Concentrations 250, 500 nM, 1, 2 µM
Incubation Time 3 days
Method

OCI-AML3 cells are co-cultured with MSCs (200000 cells/well density) and treated with CVT-10216 for 3 days in the presence or absence of recombinant TGF-β1 (5 ng/mL). ALDH activity is measured by ALDEFLUOR assay using flow cytometry.

In Vivo
In vivo

CVT-10216, a highly selective, reversible inhibitor of ALDH-2, exhibits both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety, which counteracts anxiogenic behavior induced by the benzodiazepine receptor inverse agonist in dose-dependently way.[3]

Animal Research Animal Models FH, iP and Sprague Dawley (SD) rats
Dosages 3.75, 7.5, or 15 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 465.48 Formula

C24H19NO7S

CAS No. 1005334-57-5 SDF --
Smiles C[S](=O)(=O)NC1=CC=C(C=C1)C2=COC3=C(C=CC(=C3)OCC4=CC(=CC=C4)C(O)=O)C2=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (199.79 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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