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Malotilate Lipoxygenase inhibitor

Name: Malotilate
Brand: Selleck Chemicals
SKU: S1137
Availability: InStock
Rating: 5 (1 reviews)

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.

Chemical Structure

Molecular Weight: 288.38

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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Lipoxygenase Inhibitors	ML355 PD146176 Nordihydroguaiaretic acid (NDGA) 4',5-Dihydroxyflavone AKBA (3-O-Acetyl-11-keto-β-boswellic acid) Demethylnobiletin Esculetin SR 2640 hydrochloride FPL 62064 ML351

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
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	288.38	Formula	C₁₂H₁₆O₄S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	59937-28-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NKK105			Smiles	CC(C)OC(=O)C(=C1SC=CS1)C(=O)OC(C)C

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. 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.
In vivo	Malotilate suppresses pulmonary metastasis and lung metastasis in rats. 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. 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. This compound decreases CYP2E1 levels and increases CYP2B1 levels in hepatic microsomes of rats, while CYP1A expression is not changed.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9673894/ [2] https://pubmed.ncbi.nlm.nih.gov/9652751/ [3] https://pubmed.ncbi.nlm.nih.gov/8907579/ [4] https://pubmed.ncbi.nlm.nih.gov/2825640/ [5] https://pubmed.ncbi.nlm.nih.gov/8185594/

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