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Varenicline dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Varenicline dihydrochloride图片
CAS NO:866823-63-4

CP 526555 dihydrochloride
Varenicline (CP 526555) dihydrochloride 是 α4β2 烟碱乙酰胆碱受体 (α4β2 nAChR) 的部分激动剂 其EC50值为 2.3 μM)。Varenicline dihydrochloride 是 α3β4 nAChR 和 α7 nAChR 的完全激动剂,其EC50值分别为 55 μM 和 18 μM。Varenicline dihydrochloride 是一种基于胞嘧啶结构的烟碱配体,可用于戒烟方面的研究。
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]

Cell Line:RAW 264.7 murine macrophage cells (treated with 4 μg/mL LPS for 24 h)
Concentration:1 μM
Incubation Time:0-48 h
Result:Decreased the LPS-induced cell proliferation rate.

Western Blot Analysis[4]

Cell Line:HUVECs
Concentration:1, 10, 100 μM
Incubation Time:24 h or 30 min
Result:Decreased the protein expression of VE-cadherin and activated ERK1/2, p38 and JNK signaling.
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].

Animal Model:ICR male mice[5]
Dosage:0.01-1 mg/kg for 3 days
Administration:Subcutaneous injection
Result:Inhibited nicotine conditioned place preference (CPP) in a dose dependent manner.
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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