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ML-SI3

Names

[ CAS No. ]:
891016-02-7

[ Name ]:
ML-SI3

[Synonym ]:
MFCD14811190
N-{2-[4-(2-Methoxyphenyl)-1-piperazinyl]cyclohexyl}benzenesulfonamide
Benzenesulfonamide, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]cyclohexyl]-
ML-SI3

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Cardiovascular Disease
Research Areas >> Neurological Disease

[Target]

TRPML1:4.7 μM (IC50)

TRPML2:1.7 μM (IC50)

TRPML3:12.5 μM (IC50)


[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) blocks Rapamycin (HY-10219)-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].

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
589.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H31N3O3S

[ Molecular Weight ]:
429.576

[ Flash Point ]:
310.2±32.9 °C

[ Exact Mass ]:
429.208618

[ LogP ]:
4.00

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

[ Index of Refraction ]:
1.629

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds