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Malotilate Lipoxygenase inhibitor

Cat.No.S1137

Malotilate (NKK105) is a drug used for the treatment of liver cirrhosis. This compound is a liver protein metabolism improved compound, which selectively inhibit the 5-lipoxygenase.
Malotilate Lipoxygenase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 288.38

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 288.38 Formula

C12H16O4S2

Storage (From the date of receipt)
CAS No. 59937-28-9 Download SDF Storage of Stock Solutions

Synonyms NKK105 Smiles CC(C)OC(=O)C(=C1SC=CS1)C(=O)OC(C)C

Solubility

In vitro
Batch:

DMSO : 58 mg/mL (201.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 58 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

In vitro
Malotilate at concentrations of 0.1–100 μM increases collagenase activity in a concentration-dependent manner in the multilayered cultures, but not in the monolayers. This compound increases the secretion of MMP-1 and MMP-3 in the wounded multilayered cultures, but not in the wounded monolayers. [1] It significantly reduces the invasion of the RLE monolayer by c-SST-2 cells. This chemical prevents the increase in permeability of the RLE monolayer by serum starvation. It suppresses tumour metastasis by intensifying the cell-to-cell contact of endothelial cells, thus preventing tumour cells from invading vascular endothelium. [2]
In vivo
Malotilate suppresses pulmonary metastasis and lung metastasis in rats. [2] This compound prevents increases in serum markers of type III and IV collagen synthesis as well as accumulation of the collagens, laminin and fibronectin in the liver of rats. [3] It combined with CCl4 significantly decreases hydroxyproline accumulation in the liver of rat, liver prolyl 4-hydroxylase and liver and serum galactosylhydroxylysyl glucosyltransferase activities. This chemical is also able to prevent the development of morphological changes in the liver of rats such as focal necrosis, fatty infiltration and inflammatory changes. It also normalizes almost completely the standard liver-function tests. [4] This compound decreases CYP2E1 levels and increases CYP2B1 levels in hepatic microsomes of rats, while CYP1A expression is not changed. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/2825640/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8185594/

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