1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. nAChR
  3. Varenicline Hydrochloride

Varenicline Hydrochloride (Synonyms: CP 526555 hydrochloride)

目录号: HY-10020 纯度: 98.87%
产品使用指南

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。

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Varenicline Hydrochloride Chemical Structure

Varenicline Hydrochloride Chemical Structure

CAS No. : 230615-23-3

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Other Forms of Varenicline Hydrochloride:

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  • 生物活性

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  • 参考文献

生物活性

Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist[1][2][3]. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C13H14ClN3

CAS 号
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
Varenicline Hydrochloride
目录号:
HY-10020
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