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Varenicline
Catalog No. T4246LCas No. 249296-44-4
Alias CP526555, CP 526555
Varenicline (CP 526555) is a selective partial agonist of the α4β2 nAChR and a full agonist of the α3β4 nAChR and α7 nAChR to help smokers with cardiovascular disease and COPD quit smoking.
Varenicline
Catalog No. T4246LAlias CP526555, CP 526555Cas No. 249296-44-4
Varenicline (CP 526555) is a selective partial agonist of the α4β2 nAChR and a full agonist of the α3β4 nAChR and α7 nAChR to help smokers with cardiovascular disease and COPD quit smoking.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $55 | In Stock | |
| 10 mg | $85 | In Stock | |
| 25 mg | $175 | In Stock | |
| 50 mg | $265 | In Stock | |
| 100 mg | $415 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $61 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Varenicline (CP 526555) is a selective partial agonist of the α4β2 nAChR and a full agonist of the α3β4 nAChR and α7 nAChR to help smokers with cardiovascular disease and COPD quit smoking. |
| 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.[3] |
| 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. [4] 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. [5] 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. [6] |
| Alias | CP526555, CP 526555 |
| Molecular Weight | 211.26 |
| Formula | C13H13N3 |
| Cas No. | 249296-44-4 |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | H2O: 10 mg/mL (47.34 mM), Sonication is recommended. DMSO: 10 mg/mL (47.34 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
H2O/DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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