ML-SI1 (Synonyms: DMSO : 100 mg/mL (222.53 mM; Need ultrasonic)) |
Catalog No.GC19764
One-Click Copy Product Info
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ML-SI1 es una mezcla racémica y un inhibidor del canal catiónico potencial del receptor transitorio (TRPML), con un valor de IC50 de 15μM para TRPML1
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
ML-SI1 es una mezcla racémica y un inhibidor del canal catiónico potencial del receptor transitorio (TRPML), con un valor de IC50 de 15μM para TRPML1[1, 2]. TRPML1 es un canal catiónico lisosómico involucrado en la biogénesis lisosómica, el tráfico endolisosomal (incluido el tráfico de dendritas neuronales y la autofagia [3]. ML-SI1 y ML-SI3 son actualmente los dos únicos inhibidores de TRPML publicados[4].
In vitro, el tratamiento de células PANC1 con ML-SI1 (0-100μM) durante 48h bajó la supervivencia celular e indujo cambios muy grande en el perfil metabólico[5]. El tratamiento de las neuronas del hipocampo con ML-SI1 (20μM) durante 2h bloqueó los cambios de localización lisosómica por el derribo de LAMTOR1[6]. El tratamiento de células IPEC-J2 con ML-SI1 (1.25μM) durante 24h bajó mucho los niveles de ROS y Ca2+ inducidos por AFB1, y disminuyó significativamente la apoptosis celular y la autofagia [7].
References:
[1] Reeks J, Mahajan P, Clark M, et al. High throughput cryo-EM provides structural understanding for modulators of the lysosomal ion channel TRPML1[J]. Structure, 2025.
[2] Leser C, Keller M, Gerndt S, et al. Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3[J]. European journal of medicinal chemistry, 2021, 210: 112966.
[3] Wang W, Zhang X, Gao Q, et al. TRPML1: an ion channel in the lysosome[J]. Mammalian Transient Receptor Potential (TRP) Cation Channels: Volume I, 2014: 631-645.
[4] Kriegler K, Leser C, Mayer P, et al. Effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans‐ML‐SI3[J]. Archiv der Pharmazie, 2022, 355(2): 2100362.
[5] Kim B, Jung J. Metabolomic approach to identify potential biomarkers in KRAS-Mutant pancreatic cancer cells[J]. Biomedicines, 2024, 12(4): 865.
[6] Sun J, Lin W, Hao X, et al. LAMTOR1 regulates dendritic lysosomal positioning in hippocampal neurons through TRPML1 inhibition[J]. Frontiers in Cellular Neuroscience, 2024, 18: 1495546.
[7] Cheng X, Liang J, Wu D, et al. Blunting ROS/TRPML1 pathway protects AFB1-induced porcine intestinal epithelial cells apoptosis by restoring impaired autophagic flux[J]. Ecotoxicology and Environmental Safety, 2023, 257: 114942.
| Experimentos celulares [1]: | |
Líneas celulares | Células PANC1 |
Método de preparación | Las células se trataron con ML-SI1 durante 48 horas y luego se incubaron con solución de MTT de 2 mg/ml a 37 °C en la oscuridad durante 3 horas. Después de la incubación, se añadió DMSO para disolver los cristales de formazán producidos por las células vivas. Luego se midió la absorbancia a 540 nm utilizando un lector de microplacas. |
Condiciones de reacción | 0-100μM; 48h |
Áreas de aplicación | La inhibición farmacológica de TRPML1 usando ML-SI1 disminuyó significativamente la viabilidad celular PANC1. |
References: | |
| Cas No. | SDF | ||
| Sinónimos | DMSO : 100 mg/mL (222.53 mM; Need ultrasonic) | ||
| Canonical SMILES | O=C(N1C2=CC=C(C=C2C(C1C)CCN3CCOCC3)OC)C4=C(Cl)C(Cl)=CC=C4.[Mixture of diastereomers] | ||
| Formula | C₂₃H₂₆Cl₂N₂O₃ | M.Wt | 449.37 |
| Solubility | DMSO : 100 mg/mL (222.53 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2253 mL | 11.1267 mL | 22.2534 mL |
| 5 mM | 445.1 μL | 2.2253 mL | 4.4507 mL |
| 10 mM | 222.5 μL | 1.1127 mL | 2.2253 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)