| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
ML-SA1 targets TRPML (transient receptor potential mucolipin) channels, specifically TRPML1, TRPML2, and TRPML3. It acts as a potent activator (agonist) of these lysosomal ion channels. ML-SA1 does not activate TRPM2, TRPV2, TRPV3, TRPC6, or TRPA1 channels. At 10 µM, ML-SA1 robustly activates whole cell TRPML1-4A and whole-endolysosome TRPML1, comparable to the effect of the endogenous TRPML agonist PI(3,5)P2 (1 µM).
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| ln Vitro |
It is possible that ML-SA1 (25 μM; 0–14 hours; A549 cells) will directly impact DENV2 entrance into cells [1]. Even at concentrations as high as 200 μM, ML-SA1 (0~200 μM; A549 cells) did not exhibit any cytotoxicity in cell lines. With an IC50 of 8.93 μM, ML-SA1 (0~50 μM; A549 cells) strongly suppresses DENV2 at the RNA level[1]. In A549 cells, the ML-SA1 dose model decreased ZIKV RNA and protein levels; its IC50 value for ZIKV RNA was 52.99 μM. In vitro, ML-SA1 appears to be a useful dye for DENV2 and ZIKV and functions as an activator of TRPML. In order to prevent viral infection, ML-SA1 stimulates lysosomal acidification and staining activity. ML-SA1 prevents the spread of viruses.
In vitro, ML-SA1 induces TRPML-mediated Ca2+ release from lysosomes. It reduces cholesterol accumulation in Niemann-Pick type C macrophages. ML-SA1 inhibits Dengue virus 2 and Zika virus by promoting lysosomal acidification and protease activity, with IC50 values of 8.3 µM for DENV2 RNA and 52.99 µM for ZIKV RNA. ML-SA1 can induce autophagy. |
| ln Vivo |
In vivo activity data for ML-SA1 are not extensively detailed in the available sources. The compound is used for research on lysosomal function in viral infection, where it activates lysosomal Ca2+ channels to help study virus–lysosome interactions. It may have broad-spectrum antiviral applications. Specific in vivo efficacy data in animal models have not been reported.
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| Enzyme Assay |
The in vitro assay for ML-SA1 involves measuring TRPML-mediated Ca2+ release. Cells expressing TRPML channels are loaded with a calcium-sensitive fluorescent dye (e.g., Fura-2 or Fluo-4). ML-SA1 is added at varying concentrations, and the increase in intracellular calcium is measured using fluorimetry. The compound's potency as a TRPML activator is determined from dose-response curves.
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| Cell Assay |
Western Blot analysis [1]
Cell Types: A549 cells Tested Concentrations: 25μM Incubation Duration: 0~14 hrs (hours) Experimental Results: May affect DENV2 entry into host cells. Induces autophagy in Huh7 cells or A549 cells [1]. Cellular assays for ML-SA1 are performed using macrophages, neurons, or other cell types expressing TRPML channels. Cells are treated with ML-SA1 at various concentrations. Lysosomal calcium release is measured using lysosome-targeted calcium indicators. Lysosomal acidification is assessed using pH-sensitive dyes. Autophagy is evaluated by measuring LC3-II levels and autophagosome formation. |
| Animal Protocol |
In vivo animal studies for ML-SA1 are not detailed in the available sources. The compound is used as a research tool to study TRPML channel function. Specific animal models, dosing regimens, and efficacy data have not been reported in the supplier documentation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for ML-SA1 are not available in the provided sources. The compound has a molecular weight of 362.42 g/mol and a molecular formula of C22H22N2O3. It is soluble in DMSO. The compound should be stored appropriately. Specific PK parameters such as half-life, bioavailability, and clearance have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for ML-SA1 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. The compound has been evaluated in cell-based assays at concentrations up to 10 µM for TRPML activation. Specific toxicological profiles have not been characterized.
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| References | |
| Additional Infomation |
ML-SA1 is a research compound for studying TRPML channel function in lysosomal biology, autophagy, and viral infection. It is a selective TRPML1/2/3 activator that induces lysosomal Ca2+ release. The compound is available from commercial suppliers for research use only. It can be used to study virus–lysosome interactions and broad-spectrum antiviral mechanisms.
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| Molecular Formula |
C22H22N2O3
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|---|---|
| Molecular Weight |
362.4217
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| Exact Mass |
362.163
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| CAS # |
332382-54-4
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| PubChem CID |
2880983
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| Appearance |
White to off-white solid powder
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| Density |
1.226±0.06 g/cm3
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| Boiling Point |
546.7±43.0 °C
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| LogP |
3.604
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
620
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KDDHBJICVBONAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22N2O3/c1-14-12-22(2,3)24(18-11-7-6-8-15(14)18)19(25)13-23-20(26)16-9-4-5-10-17(16)21(23)27/h4-11,14H,12-13H2,1-3H3
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| Chemical Name |
2-[2-oxo-2-(2,2,4-trimethyl-3,4-dihydroquinolin-1-yl)ethyl]isoindole-1,3-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~20.83 mg/mL (~57.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7592 mL | 13.7961 mL | 27.5923 mL | |
| 5 mM | 0.5518 mL | 2.7592 mL | 5.5185 mL | |
| 10 mM | 0.2759 mL | 1.3796 mL | 2.7592 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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