LTD4 ( Ki = 0.22±0.15 nM ); LTD4 ( Ki = 2.1±1.8 nM ); LTD4 ( pA2 = 10.5 ); LTE4 ( pA2 = 10.4 )

MK571 sodium (15 μM, 1 hour) significantly inhibits RBL-2H3 cell and mast cell composition and Ag-stimulated S1P sleep, and inhibits Fluo-3 disruption [3]. Cell Viability Assay[3] Cell Line: RBL-2H3 cells, human LAD2 mast cells Concentration: 15 μM Incubation time: 1 h Results: RBL-2H3 cells transfected with vector and SphK1 inhibited S1P secretion, but did not affect [3H]Sph Uptake and intracellular conversion of S1P. Inhibits Fluo-3 efflux, inhibits S1P export from LAD2 cells, and prevents Ag-stimulated S1P release.

MK-571 sodium (0-0.5 mg/kg, trauma, single dose) produces dose-induced transcriptional effects on the duration of induction of dyspnea in consciously sensitized individuals treated with methysergide (3 μg/kg) [1 MK-571 Sodium (0-1 mg/kg, wall, 1 dose) bursts LTD4- and Ascaris-induced fold contraction in conscious squirrel monkeys [1]. MK-571 Sodium (0-25 mg/kg, wall, 1 time). , daily, for more than 2 weeks) showed reversal of hypoxic pulmonary hypertension (PH) and protected mice from hypoxic PH [2]. Animal model: Hyperresponsive rats (male and female, 200-400 g, pre-treatment intravenous injection) 3 μg/kg methysergide, 5 minutes before antigen extraction) [1] Dosage: 0.5, 0.15 and 0.05 mg/kg Administration: Oral, once, 1 or 4 hours before challenge Results: Duration-dependent dose-dependent inhibition of antigen-induced dyspnea with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11, respectively (95% CI, 0.009-1.47) mg/kg. MK-571 was more active when administered orally as a 1% Methocel suspension (4 hours pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg. Animal model: Csnscisus squirrel msnkeys[1] Dosage: 0.1, 0.5 and 1 mg/kg Administration: Oral once 2 hours before Ascaris antigen challenge Results: 0.5 mg/kg produced significant inhibition of bronchoconstriction, produced significant inhibition 1 mg/kg inhibits the increase of RL and the decrease of Cdyn. Animal model: FVB (Friend virus type B) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) for 28 days in a ventilation chamber) [2] Dose: 0, 5, and 25 mg/kg Administration: Orally, daily, for more than 2 weeks, maintained under hypoxic conditions Results: Demonstrated reversal of hypoxic pulmonary hypertension (PH), and mice were protected from the effects of hypoxic PH. MK-571-treated mice exhibited lower RVSP and Fulton index, as well as reduced medial thickening of small pulmonary arteries and arterioles.

Cell Line: RBL-2H3 cells, human LAD2 mast cells Concentration: 15 μM Incubation Time: 1 h Result: Inhibited S1P secretion by vector and SphK1 transfected RBL-2H3 cells, whereas it did not affect uptake and intracellular conversion of [3H]Sph to S1P. Inhibited Fluo-3 efflux, inhibited S1P export by LAD2 cells, and blocked Ag-stimulated release of S1P.

Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/kg methysergide, 5 min before antigen chdlenge)
0.5, 0.15, and 0.05 mg/kg
Orally, once, 1 or 4 h before challenge

[1]. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol. 1989 Jan;67(1):17-28.

[2]. Inhibition of MRP4 prevents and reverses pulmonary hypertension in mice. J Clin Invest. 2011 Jul;121(7):2888-97.

[3]. Role of ABCC1 in export of sphingosine-1-phosphate from mast cells. Proc Natl Acad Sci U S A. 2006 Oct 31;103(44):16394-9.

C26H26CLN2NAO3S2

537.06904

536.1

C, 58.15; H, 4.88; Cl, 6.60; N, 5.22; Na, 4.28; O, 8.94; S, 11.94

115103-85-0

MK-571; 115104-28-4

Solid powder

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

XNAYQOBPAXEYLI-AAGWESIMSA-M

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+;

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

L-660,711 sodium; L660,711; MK 571; L 660,711; MK571; L-660711; L660711; L 660711; MK-571; MK-571 sodium salt

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O: ~33.3 mg/mL (~62.1 mM)
DMSO: < 1 mg/mL

Solubility in Formulation 1: ≥ 2.17 mg/mL (4.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.17 mg/mL (4.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 33.33 mg/mL (62.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)