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M7571 Sigma

MK-571 sodium salt hydrate

≥95% (HPLC)

Synonym: 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate, L-660711

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Properties

Related Categories Approved Therapeutics/Drug Candidates, Arachidonic Acid Cascade, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
InChI Key   MSHRPLRGSQECLY-DOLBFOAYSA-M
assay   ≥95% (HPLC)
form   powder
storage condition   desiccated
color   white to beige
solubility   H2O: soluble15 mg/mL, clear
originator   Merck Sharp & Dohme
shipped in   wet ice
storage temp.   −20°C

Description

Biochem/physiol Actions

MK 571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK 571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK 571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors. It potentially inhibits MRP1 and has been shown to overcome acquired arsenic tolerance.

Features and Benefits

This compound is featured on the Leukotriene Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Merck. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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Safety & Documentation

Safety Information

Symbol 
GHS07  GHS07
Signal word 
Warning
Hazard statements 
Precautionary statements 
Personal Protective Equipment 
RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis

Protocols & Articles

Articles

Discover Bioactive Small Molecules for Lipid Signaling Research

Within mammalian cells, a multitude of lipid compounds are found with a variety of cellular functions, including structural components of cell membranes and as second messengers in cell signaling pat...
Keywords: Absorption, Atomic absorption spectroscopy, Cancer, Cardiovascular, Cell signaling, Diabetes, Digestions, Diseases, Growth factors, Hormones, Inflammation, Lipid Metabolism, Lipid signaling, Metabolism

Leukotriene Receptors

Leukotrienes (LTs) exist as two distinct classes, hydroxyacids (such as LTB4), and cysteinyl leukotrienes (such as LTC4, LTD4 and LTE4). Leukotriene receptors have been classified into BLT and CysLT ...
Keywords: Addition reactions, Anti-inflammatory agents, Atomic absorption spectroscopy, Clinical, Diseases, Gene expression, Inflammation, Transduction

The Role of Inflammation in Neurodegeneration

It is well established that the brain can sense and react to peripheral insults through the rapid induction of fever and other neuroendocrine changes in response to events such as infection and tissu...
Scott Hauser, Technology Transfer Specialist, Sigma® Life Science
Biofiles, Vol. 8, No. 19
Keywords: Adhesion, Central Nervous System, Diseases, Gene expression, Inflammation, Neurodegenerative Diseases, Reductions

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