CVT-10216

Catalog No.E0355 Batch:E035501

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Technical Data

Formula

C24H19NO7S
Molecular Weight 465.48 CAS No. 1005334-57-5
Solubility (25°C)* In vitro DMSO 93 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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]

Protocol (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[3]
  • Animal Models

    FH, iP and Sprague Dawley (SD) rats

  • Dosages

    3.75, 7.5, or 15 mg/kg

  • Administration

    i.p.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.