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Varenicline dihydrochloride

Cat. No. M20984
Varenicline dihydrochloride Structure
Synonym:

Chantix, Champix

Size Price Availability Quantity
5mg USD 82  USD82 In stock
10mg USD 130  USD130 In stock
25mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.

Chemical Information
Molecular Weight 284.18
Formula C13H15Cl2N3
CAS Number 866823-63-4
Solubility (25°C) DMSO 57 mg/mL
Water 57 mg/mL
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] Başak Gke, et al. J Biochem Mol Toxicol. Association of human serum paraoxonase-1 with some respiratory drugs

[2] Michael Soyka, et al. Prog Neuropsychopharmacol Biol Psychiatry. Treatment-refractory substance use disorder: Focus on alcohol, opioids, and cocaine

[3] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

[4] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

[5] M Bays, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

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Keywords: Varenicline dihydrochloride, Chantix, Champix supplier, AChR/AChE, inhibitors, activators


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