生物活性 | |||
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描述 | TTA-A2 is a potent, selective and orally active T-type voltage gated calcium channel antagonist that reduces the activation of PXR. TTA-A2 is equally effective on Cav3.1 (a1G) and Cav3.2 (a1H) channels, with IC50 values of 89% and 89% at -80 and -100 mV holding potentials, respectively. The IC50 values at -80 and -100 mV holding potentials were 89 nM and 92 nM, respectively. TTA-A2 can be used to study a variety of human neurological disorders, including sleep disorders and epilepsy[1][2].TTA-A2 exhibits high affinity in the α1I binding assay with an affinity of 1.2 nM, and has excellent selectivity for hERG potassium channels and L-type calcium channels (both with IC50 values greater than 10 μM)[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.21mL 2.64mL 1.32mL |
26.43mL 5.29mL 2.64mL |
参考文献 |
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[1]Thomas S Reger, et al.Pyridyl amides as potent inhibitors of T-type |