Abcam, ab144303, MK 571 sodium salt (L 660711 sodium salt), CysLT1 receptor antagonist

Size: 5mg / 25mg
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.
Key facts
CAS number:115103-85-0,
Purity:>97%,
Form:SolidSee storage information,
Molecular weight:537.1 Da,
Molecular formula:C26H26ClN2NaO3S2,
PubChem:16760569,
Nature:Synthetic,
Solubility:Soluble in water to 25 mMSoluble in ethanol to 10 mMSoluble 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.