1. Metabolic Enzyme/Protease
  2. Lipoxygenase
  3. Malotilate

Malotilate (Synonyms: NKK 105)

Cat. No.: HY-A0060 Purity: 99.54%
Handling Instructions

Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=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.

For research use only. We do not sell to patients.

Malotilate Chemical Structure

Malotilate Chemical Structure

CAS No. : 59937-28-9

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Description

Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=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 (IC50)

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.
Molecular Weight

288.38

Formula

C₁₂H₁₆O₄S₂

CAS No.

59937-28-9

SMILES

O=C(OC(C)C)/C(C(OC(C)C)=O)=C1SC=CS\1

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
In Vitro: 

DMSO : ≥ 100 mg/mL (346.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MalotilateNKK 105NKK105NKK-105LipoxygenaseLOXoralanti-fibrotichepatotropicinjurycollagensynthesiscellmigrationInhibitorinhibitorinhibit

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Malotilate
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HY-A0060
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