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Purity: ≥98%
MK-571 sodium (L-660711; MK571) is a novel, potent, selective, orally bioactive antagonist of leukotriene D4 (LTD4) receptor with the potential to be used for pulmonary hypertension. It inhibits LTD4 with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes. MK-571, with Ki values of 0.22 nM and 2.1 nM, respectively, inhibits the binding of LTD4 but not LTC4 to lung membranes of guinea pigs and humans. Rats' kidney ischemia- and reperfusion-induced airway hypersensitivity are lessened by MK-571. In a mouse asthma model, MK-571 modifies the proteome of bronchoalveolar lavage fluid.
| Targets |
LTD4 ( Ki = 0.22±0.15 nM ); LTD4 ( Ki = 2.1±1.8 nM ); LTD4 ( pA2 = 10.5 ); LTE4 ( pA2 = 10.4 )
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| ln Vitro |
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.
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| ln Vivo |
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.
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| Enzyme Assay |
L-660,711 (3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl) ((3-dimethyl amino-3-oxo propyl)thio)methyl)thio)propanoic acid 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). Functionally it competitively antagonized contractions of guinea pig trachea and ileum induced by leukotriene (LT) D4 (respective pA2 values, 9.4 and 10.5) and LTE4 (respective pA2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD4 (pA2 value, 8.5). L-660,711 (5.8 x 10(-8)M) antagonized contractions of guinea pig trachea induced by LTC4 in the absence (dose ratio = 28) but not in the presence of 45 mM L-serine borate (dose ratio less than 2). L-660,711 (1.9 x 10(-5)M) did not block contractions of guinea pig trachea induced by histamine, acetylcholine, 5-hydroxytryptamine, PGF2 alpha, U-44069, or PGD2. In the presence of atropine, mepyramine, and indomethacin, L-660,711 (1.9 x 10(-5)M) inhibited a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea. L-660,711 (i.v.) antagonized bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC4, LTD4, and LTE4 but did not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal L-660,711 antagonized LTD4 (0.2-12.8 micrograms/kg)-induced bronchoconstriction in guinea pigs, and p.o. L-660,711 blocked LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 micrograms/kg). The pharmacological profile of L-660,711 indicates that it is a potent, selective, orally active leukotriene receptor antagonist which is well suited to determine the role played by LTD4 and LTE4 in asthma and other pathophysiologic conditions [1].
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| Cell Assay |
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.
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| Animal Protocol |
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 |
| References |
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| Molecular Formula |
C26H26CLN2NAO3S2
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|---|---|
| Molecular Weight |
537.06904
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| Exact Mass |
536.097
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| Elemental Analysis |
C, 58.15; H, 4.88; Cl, 6.60; N, 5.22; Na, 4.28; O, 8.94; S, 11.94
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| CAS # |
115103-85-0
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| Related CAS # |
MK-571; 115104-28-4
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| PubChem CID |
16760569
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
35
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| Complexity |
700
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C([O-])CCSC(C1=CC=CC(/C=C/C2=NC3=CC(Cl)=CC=C3C=C2)=C1)SCCC(N(C)C)=O.[Na+]
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| InChi Key |
XNAYQOBPAXEYLI-AAGWESIMSA-M
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| InChi Code |
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+;
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| Chemical Name |
3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoate
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| Synonyms |
L-660,711 sodium; L660,711; MK 571; L 660,711; MK571; L-660711; L660711; L 660711; MK-571; MK-571 sodium salt
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 Vitro) |
H2O: ~33.3 mg/mL (~62.1 mM)
DMSO: < 1 mg/mL |
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| Solubility (In Vivo) |
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. 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. View More
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. 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8620 mL | 9.3098 mL | 18.6195 mL | |
| 5 mM | 0.3724 mL | 1.8620 mL | 3.7239 mL | |
| 10 mM | 0.1862 mL | 0.9310 mL | 1.8620 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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