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CVT-10216

Cat. No. M3706
CVT-10216 Structure
Size Price Availability Quantity
10mg USD 270  USD270 In stock
25mg USD 550  USD550 In stock
50mg USD 880  USD880 In stock
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Quality Control & Documentation
Biological Activity

CVT-10216 counteracted anxiety in all models except that produced by the 5-HT(2C) agonist, mCPP. CVT-10216 exhibited both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety. CVT-10216 increases acetaldehyde after alcohol gavage and inhibits 2-bottle choice alcohol intake in heavy drinking rodents, including deprivation-induced drinking. CVT-10216 also prevents operant self-administration and eliminates cue-induced reinstatement of alcohol seeking even when alcohol is not available (i.e., no acetaldehyde). CVT-10216 prevents alcohol-induced increases in NAc DA without changing basal levels. CVT-10216 does not show rewarding or aversive properties in the CPP paradigm at therapeutic doses.

Product Citations
Chemical Information
Molecular Weight 465.48
Formula C24H19NO7S
CAS Number 1005334-57-5
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Overstreet DH, et al. Pharmacol Biochem Behav. A selective ALDH-2 inhibitor reduces anxiety in rats.

[2] Arolfo MP, et al. Alcohol Clin Exp Res. Suppression of heavy drinking and alcohol seeking by a selective ALDH-2 inhibitor.

[3] Miriam E Bocarsly, et al. The FASEB Journal. CVT-10216 selectively suppresses binge eating of palatable foods and attenuates dopamine release in the accumbens of rats

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