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• 产品描述： Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[2]. Varenicline is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment

• 靶点： EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)

• 体内研究：
  Varenicline (Subcutaneous injection, 0.01-1 mg/kg, 3 days) given 10 min prior to nicotine (0.5 mg/kg, s.c.) inhibits nicotine conditioned place preference (CPP). Varenicline (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs. Varenicline (Subcutaneous injection, 0.1 and 0.5 mg/kg, 3 days) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner

• 参考文献：
  1. Elif Baris, et al. Varenicline Prevents LPS-Induced Inflammatory Response via Nicotinic Acetylcholine Receptors in RAW 264.7 Macrophages. Front Mol Biosci. 2021 Oct 12;8:721533. 2. Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. 3. Jin H, et al. Therapeutic concentrations of varenicline in the presence of nicotine increase action potential firing in human adrenal chromaffin cells. J Neurochem. 2017 Jan;140(1):37-52. 4. Mitsuhisa Koga, 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. Toxicology. 2017 Sep 1;390:1-9. 5. Bagdas D, et al. New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology. 2018 Aug;138:72-79.

• 溶解性： DMSO  :  25  mg/mL  (118.34  mM;  Need  ultrasonic)    H2O  :  ≥  20  mg/mL  (94.67  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	4.734 ml	23.668 ml	47.335 ml
  5 mM	0.947 ml	4.734 ml	9.467 ml
  10 mM	0.473 ml	2.367 ml	4.734 ml
  50 mM	0.095 ml	0.473 ml	0.947 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *