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• 产品描述： SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.

• 靶点： pIC50: 7.1;TRP/TRPVChannel

• 体内研究：
  SB705498 exhibits potent and reversible blockade against the multiple modes of TRPV1 activation, namely the vanilloid (capsaicin), heat- and acid-mediated activation of the receptor. SB705498 displays excellent activity at 10 and 30 mg/kg po with good reversal of allodynia. SB705498 (10 mg/kg p.o.) gives 80% reversal of allodynia in the guinea pig FCA model

• 参考文献：
  1. Martin J. Gunthorpe, et al. Characterization of SB-705498, a Potent and Selective Vanilloid Receptor-1 (VR1/TRPV1) Antagonist That Inhibits the Capsaicin-, Acid-, and Heat-Mediated Activation of the Receptor. JPET June 2007 vol. 321 no. 3 1183-1192. 2. Rami HK, et al. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3287-91.

• 溶解性： DMSO  :  100  mg/mL  (232.98  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.33 ml	11.649 ml	23.298 ml
  5 mM	0.466 ml	2.33 ml	4.66 ml
  10 mM	0.233 ml	1.165 ml	2.33 ml
  50 mM	0.047 ml	0.233 ml	0.466 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 *