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ML-SI3

目录号 : GC67784

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。

ML-SI3 Chemical Structure

Cas No.:891016-02-7

规格 价格 库存 购买数量
10 mM * 1mLinDMSO
¥1,782.00
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5mg
¥1,620.00
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10mg
¥2,520.00
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25mg
¥4,680.00
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50mg
¥7,200.00
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100mg
¥10,800.00
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Sample solution is provided at 25 µL, 10mM.

Description

ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 µM and 1.7 µM respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy[1][5].

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) blocks Rapamycin -evoked ITRPML1 in 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].

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.

[1]. RÜhl P, et al. Estradiol analogs attenuate autophagy, cell migration and invasion by direct and selective inhibition of TRPML1, independent of estrogen receptors. Sci Rep. 2021 Apr 15;11(1):8313.
[2]. Kilpatrick BS, et al. Endo-lysosomal TRP mucolipin-1 channels trigger global ER Ca2+ release and Ca2+ influx. J Cell Sci. 2016 Oct 15;129(20):3859-3867.
[3]. Bais S, et al. Schistosome TRPML channels play a role in neuromuscular activity and tegumental integrity. Biochimie. 2022 Mar;194:108-117.
[4]. Zhang X, et al. Rapamycin directly activates lysosomal mucolipin TRP channels independent of mTOR. PLoS Biol. 2019 May 21;17(5):e3000252.
[5]. Xing Y, et al. Blunting TRPML1 channels protects myocardial ischemia/reperfusion injury by restoring impaired cardiomyocyte autophagy. Basic Res Cardiol. 2022 Apr 7;117(1):20.

化学性质

Cas No. 891016-02-7 SDF Download SDF
分子式 C23H31N3O3S 分子量 429.58
溶解度 DMSO : 50 mg/mL (116.39 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

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1 mg 5 mg 10 mg
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
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