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MK 571

Catalog #: 2338
5 Citations Datasheet
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2338/10
MK 571 | CAS No. 115104-28-4 | Leukotriene and Related Receptor Inverse Agonists
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Description: Potent CysLT1 (LTD4) inverse agonist. Also MRP1 inhibitor
Alternative Names: L-660711

Chemical Name: 3-[[[3-[(1E)-2-(7-Chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propanoic acid

Product Details
Citations (5)
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Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

MK 571 is a potent CysLT1 (LTD4) leukotriene receptor inverse agonist (EC50 = 1.3 nM). Antagonizes LTD4-induced contractions of guinea pig trachea and ileum (pA2 values are 9.4 and 10.5 respectively). Also inhibitor of multidrug resistance protein-1 (MRP1) mediated transport; in vitro augments the effects of cytotoxic agents on malignant cells.

Technical Data

M.Wt:
515.09
Formula:
C26H27ClN2O3S2
Solubility:
Soluble to 100 mM in DMSO
Storage:
Store at -20°C
CAS No:
115104-28-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Correlating chemical sensitivity and basal gene expression reveals mechanism of action.
    Rees M, Seashore-Ludlow B, Cheah J, Adams D, Price E, Gill S, Javaid S, Coletti M, Jones V, Bodycombe N, Soule C, Alexander B, Li A, Montgomery P, Kotz J, Hon C, Munoz B, Liefeld T, Dancik V, Haber D, Clish C, Bittker J, Palmer M, Wagner B, Clemons P, Shamji A, Schreiber S
    Nat Chem Biol, 2016;12(2):109-16.
  2. Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1.
    Vellenga et al.
    Br.J.Pharmacol., 1999;127:441
  3. Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1.
    Dupre et al.
    J.Pharmacol.Exp.Ther., 2004;309:102
  4. Involvement of LTD4 in allergic pulmonary inflammation in mice: modulation by cysLT1 antagonist MK-571.
    Blain and Sirois
    Prost.Leuko.Essent.Fatty Acids, 2000;62:361

Product Datasheets

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Citations for MK 571

The citations listed below are publications that use Tocris products. Selected citations for MK 571 include:

5 Citations: Showing 1 - 5

  1. Phosphorylation-dependent modulation of CFTR macromolecular signalling complex activity by cigarette smoke condensate in airway epithelia.
    Authors: Schnúr Et al.
    Sci Rep  2019;9:12706
  2. Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2.
    Authors: Wright Et al.
    Biochem Biophys Res Commun  2019;520:35
  3. Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters.
    Authors: Hoque Et al.
    Biochem Pharmacol  2015;59:2572
  4. A primary fish gill cell culture model to assess pharmaceutical uptake and efflux: evidence for passive and facilitated transport.
    Authors: Stott Et al.
    Antimicrob Agents Chemother  2015;159:127
  5. Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo.
    Authors: Hill Et al.
    Am J Physiol Heart Circ Physiol  2013;85:29

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