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编 号:F738712
分子式:C23H31N3O3S
分子量:429.58
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生物活性:
ML-SI3 is a mixture of cis/trans ML-SI3. ML-SI3 is a TRPML channel modulator. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 is also able to activate TRPML2 and TRPML3 with EC50s of 3.3-9.4 μM and 29 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy.

体内研究:
ML-SI3 (1.5 mg/kg, i.p., four times) attenuates I/R injury in mouse cardiomyocytes.Animal Model:Myocardial Ischemia/reperfusion (I/R) injury mice
Dosage:1.5 mg/kg
Administration:Intraperitoneal injection (i.p.), four times before and during the in vivo I/R (ischemia 30 min and reperfusion 1 day)
Result:Restored the blocked autophagic fux in the cardiomyocytes subjected to I/R.

体外研究:
ML-SI3 (10 μM) inhibits ML-SA1-evoked Ca2+ signals in HeLa cells.ML-SI3 (25-75 μM, 24h) disrupts tegumental integrity of adult schistosomes.ML-SI3 (10 μM) blocks Rapamycin (HY-10219)-evoked ITRPML1 in mimic of lysosomal lumen.ML-SI3 (3 μM, 6 h) abolishes the increase in both LC3II and p62 levels induced by hypoxia/reoxygenation (H/R) (4 h H/2 h R) in neonatal rat ventricular myocytes (NRVM).
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