生物活性 | |||
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描述 | ER-000444793, a non-toxic inhibitor of the mPTP, operates through a mechanism distinct from CypD inhibition. It effectively and in a dose-responsive manner curtails Ca2+-induced mitochondrial permeability transition (mPT). While ER-000444793 does bind to CypD, it does not displace labelled-CsA from rhCypD protein up to 50 μM, as evidenced by a CsA/CypD HTRF assay. This is in contrast to CsA and SfA, which both reduce the HTRF signal in a dose-dependent manner, indicating their displacement of labelled CsA (with IC50 values of 23 nM and 5 nM, respectively). These findings indicate that ER-000444793's ability to delay mPT is not reliant on inhibiting CypD function[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.82mL 0.56mL 0.28mL |
14.11mL 2.82mL 1.41mL |
28.22mL 5.64mL 2.82mL |
参考文献 |
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