您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Varenicline Hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Varenicline Hydrochloride
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 Hydrochloride图片
CAS NO:230615-23-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
CP 526555 hydrochloride
产品介绍
Varenicline Hydrochloride (CP 526555 Hydrochloride) 是α4β2 nAChR烟碱乙酰胆碱受体的部分激动剂 (EC50=2.3 μM)。Varenicline Hydrochloride 是 α3β4 nAChR 和 α7 nAChR 乙酰胆碱受体完全激动剂,EC50值分别为 55 μM 和 18 μM。Varenicline 是一种基于胞嘧啶结构的烟碱配体,有潜力用于戒烟方面的研究。
生物活性

Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selectiveα4β2 nicotine acetylcholine receptor (nAChR)partial agonist and fullα7nAChRagonist[1][2][3]. Varenicline Hydrochloride is also a potent partial agonist ofα6β2nAChRin striatum of rats with aKivalue of 0.12 nM[4].

IC50& Target

nAChR[1]

体内研究
(In Vivo)

Varenicline (0.5-2 mg/kg/day; subcutaneous injection; twice daily; for 14 days; male Wistar rats) treatment shows a comparable significantly higher DRD2/3 availability in the ventral striatum of approximately 11%, while only the rats treated with 1 and 2 mg/kg/day dose shows significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively. Varenicline induces dose-dependent and sustained increases in striatal DRD2/3 in rats, particularly in the ventral striatum[1].

Animal Model:Eighty male Wistar rats (250-300 g)[1]
Dosage:0.5 mg/kg/day, 1 mg/kg/day or 2 mg/kg/day
Administration:Subcutaneous injection; twice daily; for 14 days
Result:Significantly higher DRD2/3 availability in the ventral striatum of approximately 11%, while only the rats treated with 1 and 2 mg/kg/day dose showed significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively.
Clinical Trial
分子量

247.72

性状

Solid

Formula

C13H14ClN3

CAS 号

230615-23-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 50 mg/mL(201.84 mM;Need ultrasonic)

DMSO : ≥ 2.5 mg/mL(10.09 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.0368 mL20.1841 mL40.3682 mL
5 mM0.8074 mL4.0368 mL8.0736 mL
10 mM0.4037 mL2.0184 mL4.0368 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (403.68 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。