Varenicline Hydrochloride

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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。

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 aK_ivalue 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 mg

5 mg

10 mg

1 mM	4.0368 mL	20.1841 mL	40.3682 mL
5 mM	0.8074 mL	4.0368 mL	8.0736 mL
10 mM	0.4037 mL	2.0184 mL	4.0368 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。