ML-SI1 是一种非对映异构体的外消旋混合物，是一种 TRPML 抑制剂，对 TRPML1 的 IC50 值为 15 μM。
ML-SI1, a racemic mixture of diastereomers, is a TRPML inhibitor with an IC50 value of 15 μM for TRPML1.
ML-SI1 is an inseparable racemic mixture of cis-/trans-isomers (55:45) in a short synthetic sequence and its inhibitory activity on hTRPML1 (and a weak effect on TRPML2) after activation with ML-SA1. Fura-2 based single cell calcium imaging experiments confirmed that the synthesized racemic ML-SI1 (10 μM) has an inhibitory effect on hTRPML1[1].
Reference:
[1]. Charlotte Leser, et al. Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3. Eur J Med Chem. 2021 Jan 15;210:112966.
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