2418670-70-7

2418670-70-7 structure

Name: ML-SA5
Chemical Name: N'-[3-Chloro-2-(1-piperidinyl)phenyl]-N,N-dimethyl-1,4-benzenedisulfonamide
CAS Number: 2418670-70-7
Molecular Formula: C₁₉H₂₄ClN₃O₄S₂
Molecular Weight: 457.995
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2021-06-10 19:54:32
Modify Date: 2024-01-12 15:43:30
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].

Name	N'-[3-Chloro-2-(1-piperidinyl)phenyl]-N,N-dimethyl-1,4-benzenedisulfonamide
Synonyms	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-

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.