| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京