Varenicline

SKU: orb1690005

Description

Varenicline (CP 526555) is a nicotinic acetylcholine receptor ligand acting as a partial agonist at α4β2 and a full agonist at α3β4 and α7 subtypes. It is widely used in preclinical research for smoking cessation, with applications in cardiovascular and pulmonary disease models studied both in vitro and in vivo.

Research Area

Neuroscience

Key Properties

• CAS Number: 249296-44-4
• MW: 211.26
• Purity: 99.76% (May vary between batches)
• Formula: C₁₃H₁₃N₃
• SMILES: N1=CC=NC2=CC3=C(C=C12)C4CNCC3C4
• Target: AChR
• Solubility: H2O:10 mg/mL (47.34 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (4.73 mM);DMSO:10 mg/mL (47.34 mM)

Bioactivity

• In Vivo:
  Varenicline administered subcutaneously at doses of 0.5 and 1 mg/kg immediately reversed fentanyl-induced respiratory depression in rats in a dose-dependent manner and mildly alleviated the sedative effects of fentanyl. Additionally, when administered via intravenous infusion at 0.004–0.04 mg/kg/h for 23 hours per day over 7–10 days, Varenicline dose-dependently reduced self-administration of nicotine (0.0032 mg/kg/injection) alone and in combination with cocaine (0.0032 mg/kg/injection) in adult rhesus monkeys with a history of cocaine and nicotine use, without significantly affecting food-maintained responses. Moreover, Varenicline given orally at doses of 0.178–5.6 mg/kg, demonstrated antidepressant-like effects in the forced swim test in both C57BL/6J and CD-1 mice.
• In Vitro:
  Varenicline treatment at a concentration of 200 μM for 24 hours has no significant effect on the viability of HUVEC cells. At a concentration of 100 μM for 30 minutes, Varenicline significantly activates the ERK1/2 and p38 signaling pathways in HUVEC cells, which subsequently leads to reduced expression of VE-cadherin after 24 hours of treatment at the same concentration. Additionally, Varenicline treatment at 100 μM for 4 hours promotes a 2.4-fold increase in HUVEC cell migration.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP 526555, CP526555, nAChR, Varenicline

Compound Identifiers

PubChem CID

170361