ML-SI3 是一种TRPML通道抑制剂。ML-SI3 可阻断TRPML1和TRPML2,IC50s 分别为 4.7 μM 和 1.7 μM。ML-SI3 抑制溶酶体钙外流并阻断下游 TRPML1 介导的自噬。
生物活性 | ML-SI3 is aTRPMLChannel Inhibitor. ML-SI3 blocksTRPML1andTRPML2with IC50s of 4.7 μM and 1.7 μM respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction ofautophagy[1][5]. |
IC50& Target[1] | TRPML1 4.7 μM (IC50) | TRPML2 1.7 μM (IC50) | TRPML3 12.5 μM (IC50) |
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体外研究 (In Vitro) | ML-SI3 (10 μM) inhibits ML-SA1-evoked Ca2+signals in HeLa cells[2]. ML-SI3 (25-75 μM, 24h) disrupts tegumental integrity of adult schistosomes[3]. ML-SI3 (10 μM) blocksRapamycin(HY-10219)-evokedITRPML1in mimic of lysosomal lumen[4]. 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)[5].
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体内研究 (In Vivo) | ML-SI3 (1.5 mg/kg, i.p., four times) attenuates I/R injury in mouse cardiomyocytes[5].
Animal Model: | Myocardial Ischemia/reperfusion (I/R) injury mice[5] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(116.39 mM;Need ultrasonic) 配制储备液 1 mM | 2.3279 mL | 11.6393 mL | 23.2786 mL | 5 mM | 0.4656 mL | 2.3279 mL | 4.6557 mL | 10 mM | 0.2328 mL | 1.1639 mL | 2.3279 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.82 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
*以上所有助溶剂都可在本网站选购。 |