CAS NO: | 866823-63-4 |
生物活性 | Varenicline (CP 526555) dihydrochloride is a potent partial agonist forα4β2 nicotinic acetylcholine receptor (nAChR)with anEC50value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs withEC50values 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[5]. | ||||||||||||||||
IC50& Target | EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)[2] | ||||||||||||||||
体外研究 (In Vitro) | Varenicline dihydrochloride (1 μM, 24 h ) inhibits LPS-Induced cytokine secretions (IL-1β, IL-6, and TNFα) and cell proliferation rate in RAW 264.7 macrophages[1].Varenicline dihydrochloride (250 nM) evokes action potentials (Aps) in the absence of ACh stimulation in Human adrenal chromaffin cells isolated from male and female organ donors[3].Varenicline dihydrochloride (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin[4]. Cell Proliferation Assay[1]
Western Blot Analysis[4]
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体内研究 (In Vivo) | Varenicline dihydrochloride (Subcutaneous injection, 0.01-1 mg/kg, 3 days) given 10 min prior to nicotine (0.5 mg/kg, s.c.) inhibits nicotine conditioned place preference (CPP)[5].Varenicline dihydrochloride (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs[5].Varenicline dihydrochloride (Subcutaneous injection, 0.1 and 0.5 mg/kg, 3 days) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner[5].
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Clinical Trial | |||||||||||||||||
分子量 | 284.18 | ||||||||||||||||
Formula | C13H15Cl2N3 | ||||||||||||||||
CAS 号 | 866823-63-4 | ||||||||||||||||
中文名称 | 伐尼克兰二盐酸盐 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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