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• 产品描述： RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels

• 靶点： TRPM8:5.3 nM (IC50, Rat TRPM8 channels);TRPM8:8.3 nM (IC50, Human TRPM8 channels);TRPV4:10 μM (IC50);TRP/TRPVChannel

• 体外研究：
  Intracellular Ca2+ imaging reveals that menthol induced both intracellular Ca2+ release and store-operated Ca2+ entry, with RQ-00203078 inhibiting each effect. RQ-00203078 (1-10 µM) inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro

• 体内研究：
  RQ-00203078 (compound 36) demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the Icilin-induced wet-dog shakes model in rats after oral administration. Excellent oral exposure of RQ-00203078 (compound 36) is confirmed independently in rat pharmacokinetics studies at 3 mg/kg (p.o.) administration, with a Cmax value of 2300 ng/mL and 86% bioavailability

• 参考文献：
  1. Masashi Ohmi, et al. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8. 2. Yoshihiko Okamoto, et al. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int J Oncol. 2012 May;40(5):1431-40.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.802 ml	9.011 ml	18.023 ml
  5 mM	0.36 ml	1.802 ml	3.605 ml
  10 mM	0.18 ml	0.901 ml	1.802 ml
  50 mM	0.036 ml	0.18 ml	0.36 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 *