[CAS NO. 59937-28-9] Malotilate
PRODUCTS SPECIFICATIONS [59937-28-9]
DESCRIPTION [59937-28-9]
Overview
| MDL | MFCD00867646 |
|---|---|
| Molecular Weight | 288.38 |
| Molecular Formula | C12H16O4S2 |
| SMILES | O=C(OC(C)C)/C(C(OC(C)C)=O)=C1SC=CS\1 |
Summary
Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) ( IC 50 =4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes [1] [2] .
IC50 & Target
|
5-Lipoxygenase 4.7 μM (IC 50 ) |
In Vitro
Malotilate reduces collagen synthesis and cell migration activity of fibroblasts in vitro
[3]
.
Malotilate, an anti-fibrotic substance, selectively inhibited the 5-lipoxygenase, whereas both the 12- and the 15-lipoxygenase pathways are stimulated. Malotilate has been shown to prevent acute experimental liver injury induced by several hepatotoxic compounds, including Ahyl alcohot, Bromobenzene, Carbon tetrachloride, ChIoroform, Dimethylnitrosamine and Thioacetamide
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Malotilate (100 mg/kg; p.o.; daily for 3 days) treatment in rats with hypocholesterolemia results in a rapid normalization of lowered serum cholesterol [5] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male rats of the SLC-SD strain (rats with carbon tetrachloride-induced liver damage) [5] |
| Dosage: | 100 mg/kg |
| Administration: | P.o.; daily for 3 days |
| Result: | The triglyceride secretion from livers in rats given CCI4 was inhibited to about 40% of the level in the control rats. This inhibition of the triglyceride secretion was completely normalized in response to malotilate administration for 3 days. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 346.76 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Matsuda Y, et al. Effects of malotilate on alcoholic liver injury in rats. Alcohol Clin Exp Res. 1988;12(5):665-670.
- [2] Vermeer MA, Wilson JH, Zijlstra FJ, Vincent JE. Differential effects of malotilate on 5-, 12- and 15-lipoxygenase in human ascites cells. Agents Actions. 1989;26(1-2):252-253.
- [3] Poeschl A, et al. Malotilate reduces collagen synthesis and cell migration activity of fibroblasts in vitro. Biochem Pharmacol. 1987;36(22):3957-3963.
- [4] Zijlstra FJ, et al. Differential effects of malotilate on 5-, 12- and 15-lipoxygenase in human ascites cells. Eur J Pharmacol. 1989;159(3):291-295.
- [5] Wakasugi J, et al. Action of malotilate on reduced serum cholesterol level in rats with carbon tetrachloride-induced liver damage. Jpn J Pharmacol. 1985;38(4):391-401.
Synonyms
