| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Targets |
The exact molecular target of Malotilate is not clearly defined in the provided literature. It is described as an agent with antifibrotic and hepatoprotective properties. Its mechanism of action appears to involve improving hepatic function by increasing blood and bile flow and enhancing protein synthesis. It has been shown to increase collagenase activity in a concentration-dependent manner in multilayered cultures, suggesting a role in modulating the extracellular matrix, which is a key aspect of fibrosis.
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| ln Vitro |
Malotiate has the ability to decrease fibroblasts' in vitro cell migratory activity and collagen production [3]. Malotiate is an antifibrotic agent that concurrently promotes the 12- and 15-lipoxygenase pathways while selectively inhibiting 5-lipoxygenase. It has been demonstrated that malotiate protects against acute experimental liver damage brought on by a number of hepatotoxic substances, such as thioacetamide, carbon tetrachloride, ethanol, bromobenzene, and chloroform.
In vitro, Malotilate has been studied in multilayer cultures. In these systems, it increases collagenase activity in a concentration-dependent manner at concentrations ranging from 0.1 to 100 µM, without affecting monolayer cells. This suggests that its effects on collagen degradation may be dependent on the three-dimensional structure of the tissue, which is more representative of the in vivo environment. This activity is a key aspect of its potential as an antifibrotic agent. |
| ln Vivo |
Serum cholesterol levels quickly returned to normal after malotiate (100 mg/kg) was given orally to hypocholesterolemic rats once a day for three days [5].
In vivo, Malotilate has demonstrated antifibrotic and hepatoprotective properties in several animal models. It is used for the treatment of liver disease. By increasing blood and bile flow and improving protein synthesis, it aims to restore normal hepatic function. Its efficacy in models of cirrhosis and chronic hepatitis has been the basis for its investigation as a therapeutic agent for these conditions. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for Malotilate are not detailed in the provided sources. However, its activity in increasing collagenase activity suggests that it may interact with the regulatory pathways controlling matrix metalloproteinase (MMP) expression or activity. Such studies would typically involve measuring the activity of specific enzymes in the presence of the compound. The provided information suggests that its effects on collagenase activity are a key part of its mechanism.
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| Cell Assay |
In vitro cellular assays for Malotilate have been performed using multilayer cultures, which are more complex than standard monolayer cultures. In these assays, Malotilate increased collagenase activity in a concentration-dependent manner (0.1 to 100 µM). This is a key readout for its antifibrotic potential, as increased collagenase activity would lead to the degradation of excess collagen, a hallmark of fibrosis. The fact that it did not affect monolayer cells suggests a specific effect on the tissue architecture.
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| Animal Protocol |
Animal/Disease Models: SLC-SD strain male rats (rats with liver damage caused by carbon tetrachloride) [5]
Doses: 100 mg/kg Route of Administration: Po; one time/day for 3 days Experimental Results: Rats given CCI4 Hepatic triglyceride secretion was inhibited to approximately 40% of the levels in control rats. This suppression of triglyceride secretion completely normalized after 3 days of administration of malotiate. In vivo animal studies for Malotilate have been conducted in several animal models to demonstrate its antifibrotic and hepatoprotective properties. These studies typically involve inducing liver damage (e.g., via chemical toxins or surgical methods) in rodents and then administering Malotilate to assess its effects on liver function, fibrosis, and overall survival. The specific protocols and models are not detailed in the provided sources. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Malotilate are not detailed in the provided sources. It has a molecular weight of 288.38 g/mol and a molecular formula of C12H16O4S2. It is a small, lipophilic molecule. Its physical state is a solid. For research purposes, it is typically stored as a powder.
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| Toxicity/Toxicokinetics |
Malotilate is generally considered to be an agent with hepatoprotective properties. The compound is for research purposes only. While it has been studied for the treatment of liver disease, its safety and toxicity profiles would have been evaluated in preclinical and clinical studies. However, specific toxicity data are not provided in the available sources.
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| References |
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| Additional Infomation |
Malotilate is an isopropyl ester.
Malotilate is a hepatoprotective agent with antifibrotic properties. Its CAS number is 59937-28-9. It is also known by the name NKK105 and has the IUPAC name 1,3-Dithiol-2-ylidenepropanedioic acid bis(1-methylethyl) ester. It has been investigated for the treatment of cirrhosis and chronic hepatitis. It is not an approved drug in many jurisdictions and is primarily a research compound. |
| Molecular Formula |
C12H16O4S2
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|---|---|
| Molecular Weight |
288.376
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| Exact Mass |
288.049
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| CAS # |
59937-28-9
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| PubChem CID |
4006
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
321.5±42.0 °C at 760 mmHg
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| Flash Point |
138.7±15.9 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.562
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| LogP |
3.83
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
18
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YPIQVCUJEKAZCP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H16O4S2/c1-7(2)15-10(13)9(11(14)16-8(3)4)12-17-5-6-18-12/h5-8H,1-4H3
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| Chemical Name |
dipropan-2-yl 2-(1,3-dithiol-2-ylidene)propanedioate
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| Synonyms |
NKK 105; CL-1500; Malotilate
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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 : ≥ 100 mg/mL (~346.76 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.67 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 25.0 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: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4676 mL | 17.3382 mL | 34.6765 mL | |
| 5 mM | 0.6935 mL | 3.4676 mL | 6.9353 mL | |
| 10 mM | 0.3468 mL | 1.7338 mL | 3.4676 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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