Varenicline Hydrochloride

SKU: orb1703942

Description

Varenicline Hydrochloride (CP 526555) is a partial agonist of the α4β2 nicotinic acetylcholine receptor (IC50 = 250 nM). It functions as a smoking cessation aid by partially stimulating while blocking nicotine's effects, making it a key tool for in vivo and in vitro studies of nicotine dependence and addiction mechanisms.

Research Area

Neuroscience

Key Properties

• CAS Number: 230615-23-3
• MW: 247.72
• Purity: 99.85% (May vary between batches)
• Formula: C₁₃H₁₄ClN₃
• SMILES: Cl.N1=CC=NC2=CC3=C(C=C12)C4CNCC3C4
• Target: AChR,Others
• Solubility: DMSO:≥ 2 mg/mL;H2O:40 mg/mL (161.47 mM)

Bioactivity

• Target IC50:
  α4β2 nAChR:250 nM
• In Vivo:
  In rats, subcutaneous injection of Varenicline Hydrochloride (0.5, 1 mg/kg) dose-dependently reversed fentanyl-induced respiratory depression and mildly attenuated the sedative effects of fentanyl . In adult rhesus monkeys with a history of nicotine and cocaine use, continuous intravenous infusion of Varenicline Hydrochloride (0.004–0.04 mg/kg/h) for 7–10 days, 23 hours per day, dose-dependently reduced self-administration of nicotine and cocaine alone or in combination, without affecting food-rewarded operant responses . In the forced swim test with C57BL/6J and CD-1 mice, oral administration of Varenicline Hydrochloride (0.178–5.6 mg/kg) exhibited antidepressant-like effects .
• In Vitro:
  Varenicline Hydrochloride (200 μM) treatment of HUVECs for 24 hours showed no significant effect on cell viability . Varenicline Hydrochloride Hydrochloride (100 μM) significantly activated the ERK1/2 and p38 signaling pathways in HUVECs within 30 minutes, and downregulated VE-cadherin expression after 24 hours of treatment. Varenicline Hydrochloride Hydrochloride (100 μM, 4 h) enhanced HUVEC migration capacity by 2.4-fold .

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 hydrochloride, CP526555 hydrochloride, Varenicline Hydrochloride

Compound Identifiers

PubChem CID

50878597