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MK571, also known as L660711, is a potent and selective competitive inhibitor of [3H]leukotriene D4 binding in guinea pig (Ki value, 0.22 nM) and human (Ki value, 2.1 nM) lung membranes but is essentially inactive versus [3H]leukotriene C4 binding (IC50 value in guinea pig lung, 23 microM).
| ln Vitro |
MK571 (15 μM, 1 hour) drastically reduces Fluo-3 efflux and both constitutive and Ag-stimulated S1P in RBL-2H3 cells and mast cells [3].
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| ln Vivo |
Methysergide (3 μg/kg)-treated patients experience a dose-dependent inhibition of the duration of dyspnea induced at light-sensitizing concentrations when administered MK-571 (0-0.5 mg/kg once, lateral) [1]. MK-571 (0-1 mg/kg, wall, once) causes conscious squirrel monkeys to exhibit limited 4- and Ascaris-induced fold contractions [1]. MK-571 (0-25 mg/kg, wall, daily, for more than 2 weeks) counteracts the effects of hypoxic pulmonary hypertension (PH) and shields mice's chests from these effects [2].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: RBL- 2H3 cells, human LAD2 mast cells Tested Concentrations: 15 μM Incubation Duration: 1 h Experimental Results: RBL-2H3 cells transfected with vector and SphK1 inhibited S1P secretion, but did not affect [3H]Sph uptake and intracellular conversion to S1P. Inhibits Fluo-3 efflux, inhibits S1P export from LAD2 cells, and prevents Ag-stimulated S1P release. |
| Animal Protocol |
Animal/Disease Models: hyperresponsive rats (200-400 g of each male and female, pre-treatment with intravenous (iv) (iv)injection of 3 μg/kg methysergide, 5 minutes before antigen extraction) [1]
Doses: 0.5, 0.15 and 0.05 mg/kg Route of Administration: po (po (oral gavage)) once, 1 or 4 hrs (hrs (hours)) before challenge Experimental Results: Dose-dependent suppression of antigen duration-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. MK-571 was more active when administered orally as a 1% Methocel suspension (4 hrs (hrs (hours)) pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg. Animal/Disease Models: Csnscisus squirrel msnkeys[1] Doses: 0.1, 0.5 and 1 mg/kg Route of Administration: Oral once 2 hrs (hrs (hours)) before Ascaris antigen challenge Experimental 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/Disease Models: FVB (Friend virus type B) mice (Mrp4–/– and WT, 6 weeks old, exposed to chr |
| References |
[1]. Jones TR, et al. 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]. Hara Y, et al. Inhibition of MRP4 prevents and reverses pulmonary hypertension in mice. J Clin Invest. 2011 Jul;121(7):2888-97. [3]. Mitra P, et al. 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. |
| Molecular Formula |
C26H27CLN2O3S2HCL
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|---|---|
| Molecular Weight |
551.56
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| CAS # |
115104-28-4
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| Related CAS # |
MK-571 sodium;115103-85-0
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| SMILES |
CN(C)C(=O)CCSC(C1=CC=CC(=C1)/C=C/C2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8130 mL | 9.0652 mL | 18.1304 mL | |
| 5 mM | 0.3626 mL | 1.8130 mL | 3.6261 mL | |
| 10 mM | 0.1813 mL | 0.9065 mL | 1.8130 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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