Varenicline Hydrochloride
(Synonyms: 6,7,8,9-四氢-6,10-甲桥-6H-吡嗪并[2,3-H][3]苯并氮杂卓盐酸盐,CP 526555 hydrochloride) 目录号 : GC16143
Varenicline Hydrochloride (CP 526555 hydrochloride) 是一种高亲和力、选择性的 α4β2 尼古丁乙酰胆碱受体 (nAChR) 部分激动剂和完整的 α7 nAChR 激动剂。
Cas No.:230615-23-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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].
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].
References:
[1]. Crunelle CL, et al. Dose-dependent and sustained effects of varenicline on dopamine D2/3 receptor availability in rats. Eur Neuropsychopharmacol. 2011 Feb;21(2):205-10.
[2]. Kikkawa H, et al. Single- and multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy Japanese adult smokers. J Clin Pharmacol. 2011 Apr;51(4):527-37.
[3]. Pachas GN, Cather C, Pratt SA et al. Varenicline for Smoking Cessation in Schizophrenia: Safety and Effectiveness in a 12-Week, Open-Label Trial. J Dual Diagn. 2012;8(2):117-125.
[4]. Bordia T, Hrachova M, Chin M et al. Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34.
| Cas No. | 230615-23-3 | SDF | |
| 别名 | 6,7,8,9-四氢-6,10-甲桥-6H-吡嗪并[2,3-H][3]苯并氮杂卓盐酸盐,CP 526555 hydrochloride | ||
| 化学名 | (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline hydrochloride | ||
| Canonical SMILES | Cl[H].[H]C1(C([H])([H])N([H])C2([H])[H])C([H])([H])[C@]2([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13 | ||
| 分子式 | C13H14ClN3 | 分子量 | 247.72 |
| 溶解度 | Water : 50mg/mL | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。