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• 产品描述： Mavatrep is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain

• 靶点： TRP/TRPV Channel;TRP/TRPVChannel

• 体外研究：
  In cells expressing recombinant human TRPV1 channels, Mavatrep antagonized capsaicin-induced Ca2+ influx with an IC50 of 4.6 nM. Mavatrep blocked the activation of hTRPV1 channels by Capsaicin (1 μM, pH 5.0) in a concentration-dependent fashion

• 体内研究：
  In the complete Freund's adjuvant- and carrageenan-induced thermal hypersensitivity models, Mavatrep exhibited full efficacy, with ED80 values of 7.8 and 0.5 mg/kg, respectively, corresponding to plasma levels of 270.8 and 9.2 ng/mL, respectively. On the basis of Mavatrep superior pharmacologic and safety profile, Mavatrep was selected for clinical development for the treatment of pain

• 参考文献：
  1. Parsons WH, et al. Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem. 2015 May

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.367 ml	11.836 ml	23.672 ml
  5 mM	0.473 ml	2.367 ml	4.734 ml
  10 mM	0.237 ml	1.184 ml	2.367 ml
  50 mM	0.047 ml	0.237 ml	0.473 ml

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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 *