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ML-SA5

Names

[ CAS No. ]:
2418670-70-7

[ Name ]:
ML-SA5

[Synonym ]:
N'-[3-Chloro-2-(1-piperidinyl)phenyl]-N,N-dimethyl-1,4-benzenedisulfonamide
1,4-Benzenedisulfonamide, N4-[3-chloro-2-(1-piperidinyl)phenyl]-N1,N1-dimethyl-

Biological Activity

[Description]:

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 tumour growth[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Cancer

[In Vitro]

ML-SA5(1-100 μM, 24 h) 具有一定的细胞靶向特异性，在 M12 和 MeWo 细胞中可诱导大量细胞死亡，但完全保留正常黑素细胞。ML-SA5 还会导致 M12 细胞中线粒体膜电位的丧失[1]。

[In Vivo]

ML-SA5（静脉注射，2-5 mg/kg，每天，2 周）可使 MDX 小鼠的肌肉坏死减少70%以上，并减少中心有核纤维，表明 ML-SA5 可通过促进肌球蛋白修复来改善 mdx 小鼠体内的肌肉萎缩，但对 ML1 基因敲除小鼠没有作用。此外，ML-SA5 可以通过ML1 上调减少 mdx 小鼠的骨骼和心肌损伤[2]。

[References]

[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 dystrophy in mouse models. Sci Adv. 2020 Feb 7;6(6):eaaz2736.  

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
600.4±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H24ClN3O4S2

[ Molecular Weight ]:
457.995

[ Flash Point ]:
316.9±34.3 °C

[ Exact Mass ]:
457.089661

[ LogP ]:
4.73

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.623

Related Compounds