| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
MK-571 targets the cysteinyl leukotriene receptor 1 (CysLT1), which is the receptor for LTD4. It is a potent and selective competitive inhibitor of [3H]LTD4 binding in guinea pig and human lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. It blocks the binding of LTD4, but not LTC4.
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| ln Vitro |
MK571 (15 μM, 1 hour) strongly suppresses Fluo-3 efflux as well as constitutive and Ag-stimulated S1P in RBL-2H3 cells and mast cells [3].
In vitro, MK-571 is a potent antagonist of the LTD4 receptor with Kis of 0.22 nM in guinea pig and 2.1 nM in human lung membranes. It is a selective and orally active CysLT1 receptor antagonist. It is used to study the role of LTD4 in various inflammatory and allergic models. |
| ln Vivo |
MK-571 (0-0.5 mg/kg once, lateral) induces a dose-dependent decrease of the duration of dyspnea induced at light-sensitizing doses in individuals treated with methysergide (3 μg/kg) [1]. MK-571 (0-1 mg/kg, wall, once) causes modest 4- and Ascaris-induced fold contractions in awake squirrel monkeys [1]. MK-571 (0-25 mg/kg, wall, daily, for more than 2 weeks) cures hypoxic pulmonary hypertension (PH) and protects the chest of mice against the effects of hypoxia PH [2].
In vivo, MK-571 has been shown to attenuate airway hyperresponsiveness induced by renal ischemia and reperfusion in rats. As an orally active compound, it can be used in animal models to study the effects of LTD4 antagonism on various physiological and pathological processes, particularly in the respiratory system. |
| Enzyme Assay |
The in vitro receptor binding assay for MK-571 measures its ability to compete with radiolabeled LTD4 for binding to the CysLT1 receptor. Membranes from guinea pig or human lung tissue are incubated with [3H]LTD4 and varying concentrations of MK-571. The Ki values are calculated from the competition curves.
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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. In vitro cellular studies are not typical for MK-571, as its target is a receptor, and its effects are studied in tissue preparations (e.g., guinea pig ileum) or in cell lines expressing the CysLT1 receptor by measuring the inhibition of LTD4-induced calcium mobilization or other signaling events. |
| 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 In vivo animal experiments are performed in models of inflammation and allergy. For example, in a rat model, MK-571 is administered to study its effect on airway hyperresponsiveness. The compound is given orally or via other routes, and endpoints include changes in airway resistance, inflammatory cell infiltration, and levels of inflammatory mediators. |
| ADME/Pharmacokinetics |
MK-571 HCL has a molecular formula of C26H27ClN2O4S2 • HCl and a molecular weight of 551.52 g/mol. It is soluble in organic solvents like ethanol, DMSO, and DMF. It is a crystalline solid. For research, it is typically stored at -20°C. It is supplied as a research-grade compound.
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| Toxicity/Toxicokinetics |
As a potent receptor antagonist, MK-571 is not intended for human use as a research chemical. Its safety profile is not fully characterized for human use. Standard laboratory safety precautions should be followed. Its effects are related to its antagonism of the CysLT1 receptor.
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| References |
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| Additional Infomation |
MK 571 belongs to the quinoline class of compounds.
MK-571 is also known as L-660711. It is a selective, orally active CysLT1 receptor antagonist. It is a valuable tool for studying the role of leukotrienes, particularly LTD4, in inflammation, asthma, and other allergic diseases. It is available as a high-purity compound for research purposes. |
| Molecular Formula |
C26H27CLN2O3S2
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| Molecular Weight |
537.06904
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| Exact Mass |
514.115
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| CAS # |
115104-28-4
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| Related CAS # |
MK-571 sodium;115103-85-0
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| PubChem CID |
5281888
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
712.3±60.0 °C at 760 mmHg
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| Flash Point |
384.6±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.687
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| LogP |
5.93
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
34
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| Complexity |
693
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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
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| 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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