Free shipping on all orders over $ 500

Varenicline tartrate

Cat. No. M6273
Varenicline tartrate Structure
Synonym:

CP 526555-18

Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 360 In stock
100mg USD 600 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

In vitro: Varenicline is a partial agonist with 45% of nicotine's maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%.

In vivo: Varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 361.35
Formula C13H13N3·C4H6O6
CAS Number 375815-87-5
Purity 99.36%
Solubility 72 mg/mL in water
Storage at -20°C
References

Combining varenicline and nicotine patches: a randomized controlled trial study in smoking cessation.
Ramon JM, et al. BMC Med. 2014 Oct 8;12:172. PMID: 25296623.

Effects of varenicline and bupropion sustained-release use plus intensive smoking cessation counseling on prolonged abstinence from smoking and on depression, negative affect, and other symptoms of nicotine withdrawal.
Cinciripini PM, et al. JAMA Psychiatry. 2013 May;70(5):522-33. PMID: 23536105.

Effects of varenicline and bupropion sustained-release use plus intensive smoking cessation counseling on prolonged abstinence from smoking and on depression, negative affect, and other symptoms of nicotine withdrawal.
Cinciripini PM, et al. JAMA Psychiatry. 2013 May;70(5):522-33. PMID: 23536105.

Related AChR/AChE Products
Nelonicline

Nelonicline (ABT-126) is a nicotinic acetylcholine receptor agonist.

Donepezil

Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.

Atropine

Atropine (Tropine tropate) is a competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.

TD-4208

TD-4208 is a novel and potent muscarinic receptor antagonist that has a high affinity and long residence time at the M3 receptor, and demonstrates in vitro kinetic selectivity for M3 over M2 muscarinic receptor subtype and no meaningful off-target activity.

Tropicamide

Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Varenicline tartrate, CP 526555-18 supplier, AChR/AChE, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.