CP 526555 MedChemExpress (MCE)

Product Name	Varenicline
Synonyms	CS-861 Varenicline VARENICLINE 10-tetrahydro- 3-h][3]benzazepine Varenicline Impurity 7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline Synonyms CS-861 Varenicline VARENICLINE 10-tetrahydro- 3-h][3]benzazepine Varenicline Impurity 7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine
CAS	249296-44-4
EINECS
Chemical Formula	C13H13N3
Molecular Weight	211.26
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Varenicline Varenicline MedChemExpress (MCE) HY-10019 249296-44-4 CP 526555 99.92% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Varenicline Varenicline MedChemExpress (MCE) HY-10019 249296-44-4 CP 526555 99.92% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation. Varenicline (200 μM, 24 h) shows no affection to cell viability of HUVEC cells[3]. Varenicline (100 μM, 24 h) lowers expression of VE-cadherin in HUVEC cells as Varenicline (100 μM, 30 min) significantly activates ERK1/2 and p38 signaling[3]. Varenicline (100 μM, 4 h) promotes migration of HUVEC cells by 2.4-fold[3]. Varenicline (0.5, 1mg/kg, s.c., acute administration) dose-dependently reverses Fentanyl-induced respiratory depression in rats while slightly alleviates Fentanyl-induced sedation[4]. Varenicline (0.004–0.04 mg/kg/h, i.v.drip, 23h a day for 7-10 d) dose-dependently reduces self-administration of nicotine alone (0.0032 mg/kg/inj), and in combination with cocaine (0.0032 mg/kg/inj) with no significant effects on food-maintained responding in cocaine- and nicotine-experienced adult rhesus monkeys[5]. Varenicline (0.178-5.6 mg/kg, i.p., acute administration) shows antidepressant-like activity in the forced swim test in C57BL/6J and CD-1 mice[6]. EC50: 2.3 μM (α4β2 nAChR) 18 μM (α7 nAChR) 55 μM (α3β4 nAChR)[1] In Vitro Varenicline (200 μM, 24 h) shows no affection to cell viability of HUVEC cells[3]. Varenicline (100 μM, 24 h) lowers expression of VE-cadherin in HUVEC cells as Varenicline (100 μM, 30 min) significantly activates ERK1/2 and p38 signaling[3]. Varenicline (100 μM, 4 h) promotes migration of HUVEC cells by 2.4-fold[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Varenicline Related Antibodies Cell Viability Assay[3] Cell Line: HUVEC \| \| \| \| \| \| \| \| \| \| [1]. Koegelenberg CF, et al. Efficacy of varenicline combined with nicotine replacement therapy vs varenicline alone for smoking cessation: a randomized clinical trial. JAMA. 2014 Jul 312(2):155-61. [Content Brief] [2]. Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019 364(6436):eaav5282. [Content Brief] [3]. Koga M, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017 390:1-9. [Content Brief] [4]. Ren J, et al. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May 132(5):1197-1211. [Content Brief] [5]. Mello NK, et al. Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration. Neuropsychopharmacology. 2014 Apr 39(5):1222-31. [Content Brief] [6]. Rollema H, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. Eur J Pharmacol. 2009 Mar 1 605(1-3):114-6. [Content Brief]
Supplier Website	https://www.medchemexpress.com/Varenicline.html
Last Update	2025-05-21 16:50:25

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