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MK-571 sodium salt hydrate

CAS# 115103-85-0

MK-571 sodium salt hydrate

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Chemical structure

MK-571 sodium salt hydrate

3D structure

Chemical Properties of MK-571 sodium salt hydrate

Cas No. 115103-85-0 SDF Download SDF
PubChem ID 16760569 Appearance Powder
Formula C26H26ClN2NaO3S2 M.Wt 537.07
Type of Compound N/A Storage Desiccate at -20°C
Synonyms L-660711 sodium salt
Solubility DMSO : ≥ 33 mg/mL (61.44 mM)
H2O : 12.5 mg/mL (23.27 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
Chemical Name sodium;3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoate
SMILES CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)[O-].[Na+]
Standard InChIKey XNAYQOBPAXEYLI-AAGWESIMSA-M
Standard InChI 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+;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MK-571 sodium salt hydrate

DescriptionMK-571 sodium salt is a potent, selective, orally active leukotriene receptor antagonist, which inhibits [3H] LTD4 binding in guinea pig lung with a Ki of 0.22±0.15 nM and [3H]LTD4 binding in human lung with a Ki of 2.1±1.8 nM.In Vitro:MK-571 (L660,711) 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. MK-571 is essentially inactive versus [3H]LTC4 binding with IC50 values of 23±11 μM (n=16) and 32 μM (n=1) in guinea pig and human lung, respectively. MK-571 competitively antagonizes 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). MK-571 (58 nM) antagonizes 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). MK-571 (19μM) does 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, MK-571 (19 μM) inhibits a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea[1].In Vivo:MK-571 (L-660,711; i.v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC4, LTD4, and LTE4 but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 antagonizes LTD4 (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, and p.o. MK-571 blockes LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg)[1]. Hypoxia-exposed WT mice are treated with either saline or MK-571 (5 mg/kg/d or 25 mg/kg/d) for 2 more weeks while being maintain in hypoxic conditions. Saline-treated mice display all the hallmarks of PH (i.e., an increase in RVSP, Fulton index, and arterial wall thickness). However, following hypoxia, MK-571-treated mice display lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles[2].

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.

Protocol

Animal Administration [2]
Mice[2] The Mrp4-/- mice are used. Concerning the PH reversal study, 5-week-old WT mice are maintained in hypoxia for 3 weeks, then are randomized to receive, for 2 weeks, oral vehicle or MK-571 at the doses of either 5 mg/kg/d or 25 mg/kg/d. At the same time, the experiment is designed for mice in normoxia conditions. Increased hematocrit valuesare checked to assess the efficiency of hypoxia[2].

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.

MK-571 sodium salt hydrate Dilution Calculator

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MK-571 sodium salt hydrate Molarity Calculator

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Preparing Stock Solutions of MK-571 sodium salt hydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.862 mL 9.3098 mL 18.6195 mL 37.2391 mL 46.5489 mL
5 mM 0.3724 mL 1.862 mL 3.7239 mL 7.4478 mL 9.3098 mL
10 mM 0.1862 mL 0.931 mL 1.862 mL 3.7239 mL 4.6549 mL
50 mM 0.0372 mL 0.1862 mL 0.3724 mL 0.7448 mL 0.931 mL
100 mM 0.0186 mL 0.0931 mL 0.1862 mL 0.3724 mL 0.4655 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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MK-571 sodium salt hydrate

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Description

MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.

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