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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

MK 571

Cayman Chemical Item Number 10029

L 660711 (CAS 115104-28-4)

MK 571 (CAS 115104-28-4)

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Description

The cysteinyl leukotrienes (CysLTs), leukotriene (LTC4), LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the cysLT1 receptor,1 whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.2 MK 571 is a selective, orally active CysLT1 receptor antagonist.3 It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.3 MK 571 effectively blocks LTD4 activation of recombinant human and murine CysLT1 receptors1,4 but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.2,4

1 Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399 789-793 (1999).

2 Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).

3 Jones, T.R., 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 67 17-28 (1989).

4 Ogasawara, H., Ishii, S., Yokomizo, T., et al. Characterization of mouse cysteinyl leukotriene receptors mCysLT1 and mCysLT2. Differential pharmacological properties and tissue distribution. J Biol Chem 277(21) 18763-18768 (2002).

Synonyms
  • L 660711
Formal Name (E)-​3-​[[[3-​[2-​(7-​chloro-​2-​quinolinyl)ethenyl]phenyl][[3-​(dimethylamino)-​3-​oxopropyl]thio]methyl]thio]-​propanoic acid
CAS Number 115104-28-4
Molecular Formula C26H27ClN2O3S2
Formula Weight 515.1
Formulation A crystalline solid
Purity >95%
λmax 226, 283, 327, 344, 357 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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ClC1=CC=C2C(N=C(/C=C/C3=CC=CC(C(SCCC(O)​=O)​SCCC(N(C)​C)​=O)​=C3)​C=C2)​=C1

Background Reading

Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature 399 789-793 (1999).

Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).

Ogasawara, H., Ishii, S., Yokomizo, T., et al. Characterization of mouse cysteinyl leukotriene receptors mCysLT1 and mCysLT2. Differential pharmacological properties and tissue distribution. J Biol Chem 277(21) 18763-18768 (2002).

Karwatsky, J., Daoud, R., Cai, J., et al. Binding of a photoaffinity analogue of glutathione to MRP1 (ABCC1) within two cytoplasmic regions (L0 and L1) as well as transmembrane domains 10-11 and 16-17. Biochemistry 42 3286-3294 (2003).

Dallas, S., Zhu, X., Baruchel, S., et al. Functional expression of the multidrug resistance protein 1 in microglia. J Pharmacol Exp Ther 307(1) 282-290 (2003).

Jones, T.R., 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 67 17-28 (1989).

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MK 571 is available in the following screening libraries:

Size Price Quantity Subtotal
1 mg $16.00 $0.00
5 mg $72.00 $0.00
10 mg $128.00 $0.00
50 mg $560.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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