生物活性 | |||
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描述 | ICA-121431 is a nanomolar potent, broad-spectrum blocker of voltage-gated sodium channels (Nav), exhibiting particularly strong selectivity for the human Nav1.1 and Nav1.3 subtypes, with IC50 values of 13 nM and 23 nM, respectively[1]. For wild type human Nav channels, it shows IC50 values of 0.013 µM for hNav1.3, over 30 µM for hNav1.5, and 12 µM for hNav1.7, demonstrating its selective blocking capability[1]. ICA-121431 is against hNav channels with point mutations,showshNav1.3/hNav1.5 S1-S4, hNav1.3/hNav1.5 S3-S4, hNav1.3/hNav1.5 S5-S6, hNav1.3/hNav1.7 S1, hNav1.3/hNav1.7 S2, hNav1.3/hNav1.7 S3-S4, and hNav1.3/hNav1.7 S5-S6 with IC50 values of 0.083 µM, 1.2 µM, 11 µM, 2.0 µM, 0.045 µM, 0.030 µM, 0.30 µM, 1.0 µM, and 0.024 µM, respectively[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.22mL 0.44mL 0.22mL |
11.12mL 2.22mL 1.11mL |
22.24mL 4.45mL 2.22mL |
参考文献 |
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