| 产品描述： | A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter |
| 靶点： |
Nav1.8:8 nM (IC50);SodiumChannel |
| 体内研究： |
A-803467 (35 mg/kg; p.o.) shows no noticeable toxicity in the male NCR nude mice. A-803467 in combination with topotecan, significantly decreases the tumor growth in mice implanted with ABCG2 overexpressing H460/MX20 cells. A-803467 effectively restores the sensitivity of tumors overexpressing ABCG2 transporter to topotecan without having any significant effect on tumors lacking ABCG2 expression. |
| 参考文献： |
1. Anreddy N, et al. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Oncotarget. 2015;6(36):39276-39291. 2. Jarvis MF, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 2007;104(20):8520-8525. |
| 溶解性： |
DMSO : 50 mg/mL (139.75 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.795 ml |
13.975 ml |
27.949 ml |
| 5 mM |
0.559 ml |
2.795 ml |
5.59 ml |
| 10 mM |
0.279 ml |
1.397 ml |
2.795 ml |
| 50 mM |
0.056 ml |
0.279 ml |
0.559 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