| 产品描述: | 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 |
| 靶点: |
TRPML1:4.7 μM (IC50);TRPML2:1.7 μM (IC50);TRPML3:12.5 μM (IC50);GlucagonReceptor |
| 体外研究: |
ML-SI3 (10 μM) inhibits ML-SA1-evoked Ca2+ signals in HeLa cells. ML-SI3 (25-75 μM, 24h) disrupts tegumental integrity of adult schistosomes. ML-SI3 (10 μM) blocks Rapamycin (HY-10219)-evoked ITRPML1 in mimic of lysosomal lumen. 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) |
| 体内研究: |
ML-SI3 (1.5 mg/kg, i.p., four times) attenuates I/R injury in mouse cardiomyocytes. Animal Model: Myocardial Ischemia/reperfusion (I/R) injury mice 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. |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.328 ml |
11.639 ml |
23.279 ml |
| 5 mM |
0.466 ml |
2.328 ml |
4.656 ml |
| 10 mM |
0.233 ml |
1.164 ml |
2.328 ml |
| 50 mM |
0.047 ml |
0.233 ml |
0.466 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |