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AB144303

MK 571 sodium salt (L 660711 sodium salt), CysLT1 receptor antagonist

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MW 537.1 Da, Purity >97%. Potent, selective and competitive CysLT1 receptor antagonist (IC50 = 1.5 nM, LTD4). Potent MRP1 inhibitor. Shows anti-ischemic, anti-inflammatory and antinociceptive effects *in vivo.* Orally active.

View Alternative Names

AHR_HUMAN, Ah receptor, Aromatic hydrocarbon receptor, Aryl hydrocarbon receptor, Aryl hydrocarbon receptor precursor, CLTR1_HUMAN, CLTR2_HUMAN, CYSLT 1, CYSLT1R, CYSLT2, CYSLT2R, CYSLTR, CYSLTR 1, CYSLTR 2, Class E basic helix-loop-helix protein 76, CysLT(1), CysLTR vide supra, Cysteinyl leukotriene CysLT2 receptor, Cysteinyl leukotriene D4 receptor, Cysteinyl leukotriene receptor 1, Cysteinyl leukotriene receptor 2, G protein coupled receptor, G-protein coupled receptor GPCR21, G-protein coupled receptor HG55, G-protein coupled receptor HG57, GPCR, HG55, HG57, HGNC:348, HMTMF81, HPN321, LTD4 receptor, MGC46139, PSEC0146, bHLHe76, hGPCR21

1 Images
Chemical Structure - MK 571 sodium salt (L 660711 sodium salt), CysLT1 receptor antagonist (AB144303)
  • Chemical Structure

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Chemical Structure - MK 571 sodium salt (L 660711 sodium salt), CysLT1 receptor antagonist (AB144303)

2D chemical structure image of ab144303, MK 571 sodium salt (L 660711 sodium salt), CysLT1receptor antagonist

Key facts

CAS number

115103-85-0

Purity

>97%

Form

Solid

form

Molecular weight

537.1 Da

Molecular formula

C<sub>2</sub><sub>6</sub>H<sub>2</sub><sub>6</sub>ClN<sub>2</sub>NaO<sub>3</sub>S<sub>2</sub>

PubChem

16760569

Nature

Synthetic

Solubility

Soluble in water to 25 mM

Soluble in ethanol to 10 mM

Soluble in DMSO

Biochemical name

MK-571 sodium

Biological description

Potent, selective and competitive CysLT1 receptor antagonist (IC50 = 1.5 nM, LTD4). Potent MRP1 inhibitor. Shows anti-ischemic, anti-inflammatory and antinociceptive effects *in vivo.* Orally active.

Canonical smiles

CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)[O-].[Na+]

Isomeric smiles

CN(C)C(=O)CCSC(C1=CC=CC(=C1)/C=C/C2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)[O-].[Na+]

InChi

InChI=1S/C26H27ClN2O3S2.Na/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22;/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32);/q;+1/p-1/b10-6+;

InChiKey

XNAYQOBPAXEYLI-AAGWESIMSA-M

IUPAC Name

sodium;3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoate

Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
It is important to note that this product is reported to be light sensitive|Store in the dark|Store under desiccating conditions

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The Aryl hydrocarbon Receptor (AhR) known also as CysLT1 and CysLT2 is a ligand-activated transcription factor with a mass of around 96 kDa. AhR plays a pivotal role in mediating the effects of environmental toxins and endogenous compounds found within the cytosol. It transfers into the nucleus upon activation. AhR is expressed in a wide range of tissues including the liver lungs and skin. CysLT1 and CysLT2 receptors on the other hand are specific to leukotriene signaling and are mapped to cell types that are involved in the inflammatory process.
Biological function summary

AhR influences gene expression by forming a complex with the aryl hydrocarbon receptor nuclear translocator (ARNT). This complex binds DNA at xenobiotic response elements to regulate the expression of genes including CYP1A1 involved in detoxification. CysLT1 and CysLT2 receptors interact with leukotrienes which are lipid signaling molecules regulating immune responses. These receptors modulate inflammatory responses and bronchoconstriction in asthma.

Pathways

AhR plays a significant role in detoxification pathways such as the AhR signaling pathway which leads to the biotransformation and excretion of xenobiotic substances. It is also involved in regulating the immune system through interactions with other transcription factors like NF-κB. CysLT1 and CysLT2 are embedded within the leukotriene signaling pathway which involves proteins like MK-571 that inhibit CysLT1 receptor function. This is important for controlling asthma and allergic rhinitis through modulation of leukotriene activity.

AhR links to cancers and immune-related diseases due to its role in mediating responses to environmental toxins and modulating immune function. Disruptions in its signaling may lead to disorders such as liver cancer. CysLT1 and CysLT2 are connected to asthma as their over-activation contributes to the constriction of bronchial passages. MK-571 acts as an antagonist in this disease context specifically targeting CysLT1 to alleviate symptoms.

Product protocols

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