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CP-601927 

Cat. No. M29978
CP-601927  Structure
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Biological Activity

CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties.

Chemical Information
Molecular Weight 227.23
Formula C12H12F3N
CAS Number 357425-02-6
Form Liquid
Solubility (25°C) DMSO 200 mg/mL (ultrasonic)
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] Hans Rollema, et al. Psychopharmacology (Berl). The contribution of agonist and antagonist activities of α4β2* nAChR ligands to smoking cessation efficacy: a quantitative analysis of literature data

[2] Mark L Weber, et al. Neuropharmacology. Therapeutic doses of antidepressants are projected not to inhibit human α4β2 nicotinic acetylcholine receptors

[3] Sarah N Campion, et al. Birth Defects Res B Dev Reprod Toxicol. Toxicity study in juvenile rats with the α4β2 nicotinic acetylcholine receptor partial agonist CP-601,927

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Keywords: CP-601927  supplier, AChR/AChE, inhibitors, activators


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