Varenicline Tartrate
(Synonyms: 酒石酸伐尼克兰; CP 526555-18) 目录号 : GC10948
Varenicline Tartrate是一种选择性α7和α4β2烟碱型乙酰胆碱受体（nAChR）激动剂，对α4β2 nAChR的IC50值为250nM。
Cas No.:375815-87-5
Sample solution is provided at 25 µL, 10mM.
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Varenicline Tartrate is a selective α7 and α4β2 nicotinic acetylcholine receptor (nAChR) agonist with an IC50 value of 250nM for α4β2 nAChR[1]. Varenicline Tartrate is a smoking cessation drug that can reduce nicotine dependence[2, 3].
In vitro, Varenicline Tartrate (1, 10, 100μM) treatment of human umbilical vein endothelial cells (HUVEC) for 24h reduced the expression of VE-cadherin in cells and promoted cell migration[4].
In vivo, Varenicline Tartrate (0.25-1.5mg/kg, 0.178-5.6mg/kg) was intraperitoneally injected into C57BL/6J and CD-1 mice, respectively, and showed antidepressant-like activity in the forced swimming test of mice, significantly reducing the immobility of both mice[5].
References:
[1] Magnus C J, Lee P H, Bonaventura J, et al. Ultrapotent chemogenetics for research and potential clinical applications[J]. Science, 2019, 364(6436): eaav5282.
[2] Fagerström K, Hughes J. Varenicline in the treatment of tobacco dependence[J]. Neuropsychiatric Disease and Treatment, 2008, 4(2): 353-363.
[3] Faessel H M, Obach R S, Rollema H, et al. A review of the clinical pharmacokinetics and pharmacodynamics of varenicline for smoking cessation[J]. Clinical pharmacokinetics, 2010, 49(12): 799-816.
[4] Koga M, Kanaoka Y, Sugiyama K, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor–mitogen activated protein kinase axis[J]. Toxicology, 2017, 390: 1-9.
[5] Rollema H, Guanowsky V, Mineur Y S, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect[J]. European Journal of Pharmacology, 2009, 605(1-3): 114-116.
Varenicline Tartrate是一种选择性α7和α4β2烟碱型乙酰胆碱受体（nAChR）激动剂，对α4β2 nAChR的IC50值为250nM[1]。Varenicline Tartrate是一种戒烟药物，能够减少尼古丁依赖[2, 3]。
在体外，Varenicline Tartrate（1, 10, 100μM）处理人脐静脉内皮细胞（HUVEC）24h，降低了细胞中VE-钙粘蛋白的表达，促进了细胞迁移[4]。
在体内，Varenicline Tartrate（0.25-1.5mg/kg、0.178-5.6mg/kg）分别通过腹腔注射处理C57BL/6J、CD-1小鼠，在小鼠的强迫游泳实验中显示出抗抑郁样活性，显著减少了两种小鼠的静止状态[5]。
| Cell experiment [1]: | |
Cell lines | Human umbilical vein endothelial cells (HUVECs) |
Preparation Method | Cells were treated with Varenicline Tartrate (1, 10, and 100μM) for 24h, and then the expression of VE-cadherin was detected. |
Reaction Conditions | 1, 10, 100μM; 24h |
Applications | Varenicline Tartrate lowers expression of VE-cadherin in HUVECs. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice、CD-1 mice |
Preparation Method | C57BL/6J mice were treated with vehicle and Varenicline Tartrate (0.25-1.5mg/kg, i.p.). CD-1 mice were treated with vehicle, amitriptyline (10mg/kg), and Varenicline Tartrate (0.178-5.6mg/kg). The immobility time and activity time of mice were recorded every 30s for 5min and expressed as mean swimming time ± SEM. |
Dosage form | 0.25-1.5mg/kg、0.178-5.6mg/kg; i.p. |
Applications | Varenicline Tartrate significantly reduced immobility in both mouse strains. |
References: | |
| Cas No. | 375815-87-5 | SDF | |
| 别名 | 酒石酸伐尼克兰; CP 526555-18 | ||
| 化学名 | (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate | ||
| Canonical SMILES | O=C([C@]([C@@](C(O[H])=O)([H])O[H])([H])O[H])O[H].[H][C@@]12C([H])([H])C(C([H])([H])N([H])C2([H])[H])([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13 | ||
| 分子式 | C13H13N3.C4H6O6 | 分子量 | 361.35 |
| 溶解度 | ≥ 18.07mg/mL in DMSO, ≥ 96.2 mg/mL in Water | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7674 mL | 13.837 mL | 27.674 mL |
| 5 mM | 0.5535 mL | 2.7674 mL | 5.5348 mL |
| 10 mM | 0.2767 mL | 1.3837 mL | 2.7674 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet