MK-571 sodium salt

SKU: orb1226905

Description

A potent and specific LTD4 receptor antagonist with Ki of 0.22 nM; effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors; also is an inhibitor of multidrug resistance protein-1 (MRP1) mediated transportorally active.Asthma Phase 2 Clinical(In Vitro):MK571 (15 μM, 1 h) sodium markedly suppresses constitutive and Ag-stimulated S1P secretion from RBL-2H3 cells and mast cells, and inhibits Fluo-3 efflux.(In Vivo):MK-571 sodium (0-0.5 mg/kg, orally, once) produces dose-dependent inhibition of the duration of antigen-induced dyspnea in conscious sensitized rats treated with methysergide (3 μg/kg).MK-571 sodium (0-1 mg/kg, orally, once) blocks LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys.MK-571 sodium (0-25 mg/kg, Orally, daily, for 2 more weeks) shows reversal of hypoxic pulmonary hypertension (PH), and protects mice from hypoxic PH.

Key Properties

• CAS Number: 115103-85-0
• MW: 537.069
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₆ClN₂NaO₃S₂
• SMILES: CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)[O-].[Na+]
• Target: Leukotriene Receptor
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vivo:
  Animal model: Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/kg methysergide, 5 min before antigen chdlenge). Dosage: 0.5, 0.15, and 0.05 mg/kg. Administration: Orally, once, 1 or 4 h before challenge. Result: Produced dose-dependent inhibition of the duration of antigen-induced dyspnea, with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11 (95% CI, 0.009-1.47) mg/kg, respectively. MK-571 was even more active when administered orally as a suspension in 1% Methocel (4 h pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg. Animal model: Csnscisus squirrel msnkeys. Dosage: 0.1, 0.5, and 1 mg/kg. Administration: Orally, once, 2 h prior to challenge with Ascaris antigen. Result: Produced significant inhibition of the bronchoconstriction at 0.5 mg/kg, produced significant inhibition of the increases in RL and decreases in Cdyn at 1 mg/kg. Animal model: FVB (Friend virus B-type) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) in a ventilated chamber for 28 days). Dosage: 0, 5, and 25 mg/kg. Administration: Orally, daily, for 2 more weeks, maintain in hypoxic conditions. Result: Showed reversal of hypoxic pulmonary hypertension (PH), and mice were protected from hypoxic PH. MK-571-treated mice displayed lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

L-660711 sodium salt

Quick Database Links

Gene Symbol

Leukotriene Receptor