A selective, reversible ALDH2 inhibitor
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Product Type

Small Molecule Modulators
Small Molecule Inhibitors

Research Area

CVT-10216

Item No. 18318

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[3-[4-[(methylsulfonyl)amino]phenyl]-4-oxo-4H-1-benzopyran-7-yl]oxy]methyl]-benzoic acid
CAS Number
1005334-57-5
Synonyms
  • GS-455534
Molecular Formula
C24H19NO7S
Formula Weight
465.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 20 mg/ml
λmax
234, 259 nm
SMILES
OC(C1=CC=CC(COC2=CC=C(C(C(C3=CC=C(NS(C)(=O)=O)C=C3)=CO4)=O)C4=C2)=C1)=O
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)
InChi Key
YYOOFJZTRCPVFD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Aldehyde dehydrogenase 2 (ALDH2) is a mitochondrial enzyme involved in the major oxidative pathway of alcohol metabolism. CVT-10216 is a reversible inhibitor of ALDH2 (IC50 = 29 nM) that demonstrates >40-fold selectivity for ALDH2 over the cytosolic isoform, ALDH1.1 CVT-10216 has been reported to reduce excessive alcohol drinking in alcohol-preferring rats and to prevent self-administration of alcohol in Long-Evans rats.1 This compound has also been shown to produce anxiolytic effects in four different rodent models, including a model of repeated alcohol withdrawal-induced anxiety.1 The efficacy of CVT-10216 has also been examined in rodent models of drug addiction or binge eating of high-fat or high-sugar diets.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Overstreet, D.H., Knappa, D.J., Breese, G.R., et al. A selective ALDH-2 inhibitor reduces anxiety in rats. Pharmacol. Biochem. Behav. 94(2), 255-261 (2009).

    2. Bocarsly, M.E., Hoebel, B.G., Paredes, D., et al. GS 455534 selectively suppresses binge eating of palatable food and attenuates dopamine release in the accumbens of sugar-bingeing rats. Behav.Pharmacol. 25(2), 147-157 (2014).