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MK-571 sodium

Catalog No. T3148 CAS 115103-85-0

Synonyms: Verlukast sodium, MK571, L-660711 sodium salt, MK-571 sodium salt, L-660711 (sodium salt), L-660711, Propanoic acid

MK-571 is a selective, orally active antagonist of the CysLT1 receptor. MK571 is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK571 can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK571 significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

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MK-571 sodium, CAS 115103-85-0

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Purity: 98%

Biological Description

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Description	MK-571 is a selective, orally active antagonist of the CysLT1 receptor. MK571 is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK571 can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK571 significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.
Targets&IC50	LTD 4:2.1 nM (Ki, In human lung), LTD 4:0.22 nM (Ki, In guinea pig lung)
Cell Research	Cells were seeded onto 96 well plates at a concentration of 1×103 cells per well and incubated for 72 h at 37?C and 5% CO2 to allow MRP1 messenger RNA suppression to occur. Cells were then treated with either control media or one of three chemotherapy drugs temozolomide (150 µM), vincristine (100 nM), or etoposide (2 µM). Cells were then returned to the incubator for a further 72 h; after which time, Metylthiazol Tetrazolium (MTT) powder in PBS (50µl of 5 mg/ml) was added to each well. Cells were then incubated for a further 4 h after which all solution was removed and dimethyl sulfoxide (DMSO) was added. After 10 min incubation time at 37?C, absorbance was recorded at 570 nm wavelength and data was recorded and analyzed. Small molecule inhibitors MK571 (25 µM) and Reversan (15µM) were added 7 h prior to carrying out further drug treatment (temozolomide, vincristine or etoposide) or assay assessment (media change for proliferation and 2D-migration assays) (Only for Reference)

Synonyms	Verlukast sodium, MK571, L-660711 sodium salt, MK-571 sodium salt, L-660711 (sodium salt), L-660711, Propanoic acid
Molecular Weight	537.07
Formula	C26H27ClN2O3S2·Na
CAS No.	115103-85-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 93 mg/mL (173.2 mM)

Ethanol: 16 mg/mL (29.8 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Jones TR, et al. Can J Physiol Pharmacol. 1989, 67(1):17-28. 2. Amanda Tivnan, et al. Front Neurosci. 2015, 9:218. 3. Depré M, et al. Eur J Clin Pharmacol. 1992, 43(4):427-30. 4. Luo FR, et al. Drug Metab Dispos. 2002, 30(7):763-70.

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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.

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Keywords

MK-571 sodium 115103-85-0 GPCR/G Protein Immunology/Inflammation LTR Leukotriene Receptor MRP4 Lysophospholipid Receptor human mast cells LAD2 Verlukast sodium MK 571 sodium MRP1 MK571 sphingosine kinase L660711 ABCC1 LPL Receptor bronchoconstriction Sphingolipids L-660711 sodium salt Inhibitor MK-571 MK-571 sodium salt L-660711 (sodium salt) L 660711 L-660711 ATP-binding cassette pulmonary hypertension inhibit dyspnea MK571 sodium RBL-2H3 cells MK 571 Propanoic acid inhibitor

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