MK-571 sodium salt hydrate - CAS 115103-85-0
Catalog number: 115103-85-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H26ClN2NaO3S2
Molecular Weight:
537.07
COA:
Inquire
Targets:
Leukotriene Receptor
Description:
The sodium salt hydrate of MK-571 which is an effective antagonist of CysLT1 receptor and an inhibitor of MRP1.
Purity:
95%
Related CAS:
115104-28-4 (free acid)
Appearance:
Solid powder
Synonyms:
sodium (E)-3-(((3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)((3-(dimethylamino)-3-oxopropyl)thio)methyl)thio)propanoate; MK-571; MK 571; MK571; MK-571 sodium salt; L-660,711; L660,711; L 660,711; L-660711; L660711; L 660711
Solubility:
DMSO: ≥ 33 mg/mL
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
The sodium salt hydrate of MK-571 which is an effective antagonist of CysLT1 receptor and an inhibitor of MRP1.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
XNAYQOBPAXEYLI-AAGWESIMSA-M
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+;
Canonical SMILES:
O=C([O-])CCSC(C1=CC=CC(/C=C/C2=NC3=CC(Cl)=CC=C3C=C2)=C1)SCCC(N(C)C)=O.[Na+]
1.Uptake and metabolism of sulphated steroids by the blood-brain barrier in the adult male rat.
Qaiser MZ;Dolman DEM;Begley DJ;Abbott NJ;Cazacu-Davidescu M;Corol DI;Fry JP J Neurochem. 2017 Sep;142(5):672-685. doi: 10.1111/jnc.14117. Epub 2017 Aug 3.
Little is known about the origin of the neuroactive steroids dehydroepiandrosterone sulphate (DHEAS) and pregnenolone sulphate (PregS) in the brain or of their subsequent metabolism. Using rat brain perfusion in situ, we have found ;3; H-PregS to enter more rapidly than ;3; H-DHEAS and both to undergo extensive (> 50%) desulphation within 0.5 min of uptake. Enzyme activity for the steroid sulphatase catalysing this deconjugation was enriched in the capillary fraction of the blood-brain barrier and its mRNA expressed in cultures of rat brain endothelial cells and astrocytes. Although permeability measurements suggested a net efflux, addition of the efflux inhibitors GF120918 and/or MK571 to the perfusate reduced rather than enhanced the uptake of ;3; H-DHEAS and ;3; H-PregS; a further reduction was seen upon the addition of unlabelled steroid sulphate, suggesting a saturable uptake transporter. Analysis of brain fractions after 0.5 min perfusion with the ;3; H-steroid sulphates showed no further metabolism of PregS beyond the liberation of free steroid pregnenolone. By contrast, DHEAS underwent 17-hydroxylation to form androstenediol in both the steroid sulphate and the free steroid fractions, with some additional formation of androstenedione in the latter.
2.Bronchodilation with a potent and selective leukotriene D4 (LTD4) receptor antagonist (MK-571) in patients with asthma.
Gaddy JN;Margolskee DJ;Bush RK;Williams VC;Busse WW Am Rev Respir Dis. 1992 Aug;146(2):358-63.
The sulfidopeptide leukotrienes LTC4, LTD4, and LTE4 can cause airway smooth muscle contraction and have been implicated in the pathophysiology of asthma. MK-571 is a selective, potent LTD4 receptor antagonist that could attenuate airway obstruction in asthma by inhibiting the actions of sulfidopeptides at the LTD4 receptor site. The objectives of this study were to investigate the potential for MK-571 to cause bronchodilation in asthma patients with existing airway obstruction and to evaluate its effect on the bronchodilation response to an inhaled beta 2-agonist (albuterol). Twelve male patients (ages 19 to 42 yr) with asthma (baseline FEV1 50 to 80% predicted) participated in this placebo-controlled, randomized, two-period, cross-over study. On separate treatment days, each patient received either MK-571 or placebo intravenously for 6 h; inhaled albuterol was administered at the fifth and sixth hour of MK-571/placebo treatment to achieve maximal bronchodilation on that study day. Spirometry (forced expiratory volume in 1 s, FEV1) was monitored at intervals throughout each study period. MK-571 caused clinically significant bronchodilation; the increase in FEV1 above baseline, 20 min after the start of the MK-571 infusion, was 22 +/- 3.
3.Evaluation and comparison of MRP1 activity with three fluorescent dyes and three modulators in leukemic cell lines.
Dogan AL;Legrand O;Faussat AM;Perrot JY;Marie JP Leuk Res. 2004 Jun;28(6):619-22.
MRP1 activity was evaluated and compared in 11 cell lines with different levels of MRP1 expression using functional assays of calcein acetoxymethyl ester (calcein-AM), carboxyfluorescein diacetate (CFDA) and Rhodamine 123 (Rh123) in combination with the modulators cyclosporin A (CsA), probenecid and MK571. A good correlation was found between MRP1 expression and the modulatory effect of MK571 on calcein-AM uptake (P = 0.01 and probenecid effect on CFDA uptake (P = 0.02). Additionally, the combined modulatory effect of MK571 and probenecid on CFDA uptake (P < 0.0001) and on calcein-AM uptake (P = 0.0001) were highly significant. No correlation was found between MRP1 expression and the effects of three modulators on Rh123 uptake or efflux. In conclusion, calcein-AM and CFDA uptake assays are the best choices to probe MRP1 activity and combination of two modulators may improve the efficiency of these assays.
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