MK 571 (Synonyms: L-660,711) |
Catalog No.GC12197 |
leukotriene D4 receptor antagonist, orally active
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 115104-28-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
U937 cell line |
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions |
IL-6 protein determination: Freshly isolated monocytes were stimulated with medium, LPS (1 ng/ml), MK-571 (10 μM), and the combination of both during 24 h. |
Applications |
Costimulating the cells with 10 μM MK-571 and 1 ng/ml LPS enhanced IL-6 secretion(2.0±0.4 fold increase, p<0.01)than cells only stimulated by LPS. And a 1.6 fold increase in IL-6 mRNA expression was also observed by the combination of LPS and MK-571 compared to the effects of LPS alone. |
Animal experiment [2]: | |
Animal models |
Sensitized male Balb/c mice weighing 20±25 g |
Dosage form |
Effect of MK-571on cell infiltration: Animals were treated with an injection of MK-571 in the caudal vein (1, 10, 100 mg/kg ) for 30 min |
Applications |
The MK-571 inhibition for eosinophil infiltration in the bronchoalveolar lavage was 46%, 63.9% and 90% at the dose of 1 mg/kg, 10 mg/kg and 100 mg/kg. And MK-571 produced a total inhibition of neutrophil infiltration. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Edo Vellenga, Leonore Tuyt, Bart-Jan Wierenga, Michael Muller & Wim Dokter. Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specifc inhibitor of the multi-drug resistance protein-1. Br J Pharmacol, 1999, 127(2): 441-448. [2]. Blain JF, Sirois P. Involvement of LTD(4) in allergic pulmonary inflammation in mice: modulation by cysLT(1)antagonist MK-571. Prostaglandins Leukot Essent Fatty Acids, 2000, 62(6): 361-368. |
MK 571 (L-660,711) is a novel potent and selective antagonist of leukotriene D4 receptor with Ki values of 0.22 nM and 2.1 nM in guinea pig and human lung membranes, respectively [1]. MK 571 is also a specific inhibitor of the multidrug resistance protein 1 (MRP1) [2].
Leukotriene D4 (LTD4) is one of the leukotrienes and is released by basophils. LTD4 induces the contraction of smooth muscle and increases vascular permeability. Cysteinyl leukotriene receptor 1 (cysLT1 receptor, LTD4 receptor) is a G protein-coupled receptor activated by LTD4 [3].
MK 571 (L-660,711) is a potent, selective and orally active leukotriene D4 receptor antagonist. MK 571 competitively antagonized contractions of guinea pig trachea and ileum induced by LTD4 (pA2 values, 9.4 and 10.5) and LTE4 (pA2 values, 9.1 and 10.4) , and antagonized contractions of human trachea induced by LTD4 with pA2 value of 8.5 [1].
In anesthetized guinea pigs, MK 571 antagonized bronchoconstriction induced by LTC4, LTD4, and LTE4 [1]. In mice, MK 571 (1, 10, 100 mg/kg) inhibited inflammatory cell infiltration in the bronchoalveolar lavage in a dose-dependent way with maximal inhibition of 90%. MK 571 also inhibited bronchial hyperreactivity and reduced lung microvascular leakage by 22% at 10 mg/kg [3].
References:
[1]. Jones TR, Zamboni R, Belley M, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol, 1989, 67(1): 17-28.
[2]. Vellenga E, Tuyt L, Wierenga BJ, et al. Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1. Br J Pharmacol, 1999, 127(2): 441-448.
[3]. Blain JF, Sirois P. Involvement of LTD(4) in allergic pulmonary inflammation in mice: modulation by cysLT(1)antagonist MK-571. Prostaglandins Leukot Essent Fatty Acids, 2000, 62(6): 361-368.
Cas No. | 115104-28-4 | SDF | |
Synonyms | L-660,711 | ||
Chemical Name | (R,E)-3-(((3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)((3-(dimethylamino)-3-oxopropyl)thio)methyl)thio)propanoic acid | ||
Canonical SMILES | ClC1=CC=C2C(N=C(C=C2)/C=C/C3=CC([C@@H](SCCC(O)=O)SCCC(N(C)C)=O)=CC=C3)=C1 | ||
Formula | C26H27ClN2O3S2 | M.Wt | 515.09 |
Solubility | <5.15mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.9414 mL | 9.707 mL | 19.4141 mL |
5 mM | 0.3883 mL | 1.9414 mL | 3.8828 mL |
10 mM | 0.1941 mL | 0.9707 mL | 1.9414 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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