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 |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.