Varenicline-d₄ hydrochloride

Cat. No.: HY-10019AS1: FAQs
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Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A). Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment.

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Varenicline-d<sub>4</sub> hydrochloride Chemical Structure

Varenicline-d₄ hydrochloride Chemical Structure

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2500 μg	USD 575	In-stock	Estimated Time of Arrival: December 31

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description	Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A)^[1]. Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively^[2]. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment^[3].
In Vitro	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Varenicline-d₄ hydrochloride Related Antibodies
Formula	C₁₃H₉D₄N₃.xHCl
SMILES	[2H]C1([2H])C2C3=CC4=NC=CN=C4C=C3C(C2)C([2H])([2H])N1.Cl.[x]
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (277 KB) Handling Instructions (2659 KB)
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-246. [Content Brief] [2]. Elif Baris, et al. Varenicline Prevents LPS-Induced Inflammatory Response via Nicotinic Acetylcholine Receptors in RAW 264.7 Macrophages. Front Mol Biosci. 2021 Oct 12;8:721533. [Content Brief] [3]. Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [Content Brief] [4]. Jin H, et al. Therapeutic concentrations of varenicline in the presence of nicotine increase action potential firing in human adrenal chromaffin cells. J Neurochem. 2017 Jan;140(1):37-52. [5]. Mitsuhisa Koga, 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 Sep 1;390:1-9. [Content Brief] [6]. Bagdas D, et al. New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology. 2018 Aug;138:72-79. [Content Brief]