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Varenicline-15N,13C,d2

Varenicline-15N,13C,d2

Item no.	HY-10019S1
Manufacturer	MedChem Express
Amount	1 ea
Specific against	other
Citations	[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.<br/>[2]Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364(6436):eaav5282.<br/>[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.<br/>[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.<br/>[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.<br/>[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.<br/>[7]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
Smiles	[2H]C1([2H])[15NH][13CH2]C2CC1C3=C2C=C4N=CC=NC4=C3
Alias	CP 526555-15N,13C,d2
Available
Product Description	Varenicline-15N, 13C, d2 is 15N and deuterated labeled Varenicline (HY-10019). 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[1][2][3][4][5].
Shipping	Room temperature
Manufacturers Applications	COVID-19-immunoregulation
MolecularWeight	215.26
Clinical Information	No Development Reported
Manufacturers Research Area	Cancer; Inflammation/Immunology; Neurological Disease
Solubility	10 mM in DMSO
Target	Isotope-Labeled Compounds; nAChR
Manufacturers Target	Isotope-Labeled Compounds; nAChR
Manufacturers Pathway	Membrane Transporter/Ion Channel; Neuronal Signaling; Others
Manufacturers Product type	Isotope-Labeled Compounds

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