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-SI1은 외소성 혼합물이고 일시적 수용체 전위 카티온 채널 (TRPML)의 억제제로 TRPML1에 대한 IC50 값은 15μM이다.
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-SI1은 외소성 혼합물이고 일시적 수용체 전위 카티온 채널 (TRPML)의 억제제로 TRPML1에 대한 IC50 값은 15μM이다. TRPML1은 리소좀 생성, 엔도리소좀 수송 (신경 원소수 속의 수송 포함) 그리고 자가포식에 관여하는 리소좀 카티온 채널이다[3]. ML-SI1과 ML-SI3은 현재까지 발표된 유일한 두 가지 TRPML 억제제이다[4].
체외 실험에서 ML-SI1 (0-100μM)으로 PANC1 세포를 48시간 처리하면 세포 생존율을 현저하게 감소시키고 대사 프로필에 유의한 변화를 유도한다[5]. ML-SI1 (20μM)으로 해마 신경세포를 2시간 처리하면 LAMTOR1 경매에 의해 유도된 리소좀 위치 변화를 차단한다[6]. ML-SI1 (1.25μM)으로 IPEC-J2 세포를 24시간 처리하면 AFB1에 의해 유도된 ROS와 Ca2+ 수준을 현저하게 감소시키고 세포 사멸과 자식을 현저하게 줄인다[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.
| 세포 실험 [1]: | |
세포 라인 | PANC1 세포 |
제조 방법 | 세포를 ML-SI1로 48시간 처리한 후 37°C에서 어두운 곳에서 2mg/mL MTT 용액과 3시간 동안 공진시켰습니다. 공진 후 생존한 세포가 생성한 포르말라잔 결정을 녹이기 위해 DMSO를 추가하였습니다. 이 후에 미세 플레이트 리더를 사용하여 540nm에서 흡광도를 측정하였습니다. |
반응 조건 | 0-100μM; 48 시간 동안 |
응용 분야 | ML-SI1을 사용한 TRPML1의 약리학적 억제는 PANC1 세포 생존율을 현저하게 감소시켰습니다. |
References: | |
| Cas No. | SDF | ||
| Synonyms | 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.)