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CVT 10216

Names

[ CAS No. ]:
1005334-57-5

[ Name ]:
CVT 10216

[Synonym ]:
Benzoic acid, 3-[[[3-[4-[(methylsulfonyl)amino]phenyl]-4-oxo-4H-1-benzopyran-7-yl]oxy]methyl]-
3-{[(3-{4-[(Methylsulfonyl)amino]phenyl}-4-oxo-4H-chromen-7-yl)oxy]methyl}benzoic acid
CVT-10216

Biological Activity

[Description]:

CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduces excessive alcohol drinking in alcohol-preferring rats and exhibits anxiolytic effects[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Aldehyde Dehydrogenase (ALDH)
Research Areas >> Neurological Disease

[Target]

IC50: 29 nM (ALDH-2)[1]


[In Vivo]

CVT-10216 (intraperitoneal injection; 3.75, 7.5, or 15 mg/kg) exhibits a increase in social interaction as a dose-dependent manner, punctuated by a 2-fold increase in social interaction after 15 mg/kg in Fawn-Hooded rats[1]. CVT-10216 (intraperitoneal injection; 3.75 or 15 mg/kg) are determined 5 h into the third withdrawal.It has the anxiolytic effect of 15 mg/kg CVT-10216 in this model, but has no significant effects on locomotor activity[1].

[References]

[1]. Overstreet DH, et al. A selective ALDH-2 inhibitor reduces anxiety in rats.Pharmacol Biochem Behav. 2009 Dec;94(2):255-61.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
714.2±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H19NO7S

[ Molecular Weight ]:
465.475

[ Flash Point ]:
385.8±35.7 °C

[ Exact Mass ]:
465.088226

[ PSA ]:
131.29000

[ LogP ]:
3.55

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.676

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Related Compounds