ML-SA5
目录号 : GC69478ML-SA5 是一种强效的 TRPML1 阳离子通道激动剂,能激活 DMD 肌细胞中的整个内溶体 TRPML1(ML1)电流,EC50 值为 285 nM ,其效力高于 ML-SA1。ML-SA5 具有抗癌活性,可以抑制肿瘤生长。
Cas No.:2418670-70-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ML-SA5 is a potent TRPML1 cation channel agonist that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and is more potent than ML-SA1. ML-SA5 has anticancer activity and can inhibit tumour growth[1].
ML-SA5(1-100 μM, 24 h) has some cell-targeting specificity and induces substantial cell death in M12 and MeWo cells, but fully preserves normal melanocytes. It also causes a loss of mitochondrial membrane potential in M12 cells[1].
ML-SA5 (i.p., 2-5 mg/kg, daily, 2 weeks) reduces muscle necrosis in MDX mice by more than 70% and reduces central nucleated fibers, suggesting that ML-SA5 can improve muscle atrop in mdx mice in vivo by promoting myosin repair, but has no effect in ML1 knockout mice. Moreover, ML-SA5 reduces skeletal and cardiac muscle damage in mdx mice through ML1 upregulation[2].
[1]. Wanlu Du, et al. Lysosomal Zn2+release triggers rapid, mitochondria-mediated, non-apoptotic cell death in metastatic melanoma. Cell Rep. 2021 Oct 19;37(3):109848.
[2]. Lu Yu, et al. Small-molecule activation of lysosomal TRP channels ameliorates Duchenne muscular dystrop in mouse models. Sci Adv. 2020 Feb 7;6(6):eaaz2736.
Cas No. | 2418670-70-7 | SDF | Download SDF |
分子式 | C19H24ClN3O4S2 | 分子量 | 457.99 |
溶解度 | DMSO : 125 mg/mL (272.93 mM; Need ultrasonic) | 储存条件 | Store at -20°C,protect from light |
General tips | 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°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。 |
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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。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1835 mL | 10.9173 mL | 21.8345 mL |
5 mM | 0.4367 mL | 2.1835 mL | 4.3669 mL |
10 mM | 0.2183 mL | 1.0917 mL | 2.1835 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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