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MK-571 (sodium salt) (CAS 115103-85-0) LS-H161

CysLT1 receptor antagonist
LS-H161-1 / 1 mg / $175
LS-H161-5 / 5 mg / $195
LS-H161-10 / 10 mg / $225
LS-H161-50 / 50 mg / $425
USA Shipment Only
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Description: The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the cysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK-571 is a selective, orally active CysLT1 receptor antagonist. 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. MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or mouse CysLT2 receptors. H161_ChemicalStructureImage.png
(E)-3-[[[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]-propanoic acid, sodium salt
L-660,711
biochemical, chemical, antagonist
LS-H161
115103-85-0
C26H26ClN2O3S2 • Na
≥95%
A crystalline solid
 
CCCSC(SCCC(=O)N(C)C)c1cccc(\C=C/c2ccc3ccc(Cl)cc3n2)c1
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+;
XNAYQOBPAXEYLI-AAGWESIMSA-M
Shipped Ambient, store at -20°C, ≥ 1 year shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CYSLTR1 / CYSLT1 related products

Usage Information

MK-571 (sodium salt) is supplied as a crystalline solid. A stock solution may be made by dissolving the MK-571 (sodium salt) in an organic solvent purged with an inert gas. MK-571 (sodium salt) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of MK-571 (sodium salt) in ethanol is approximately 1 mg/ml, and it is approximately 10 mg/ml in DMSO and DMF. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of MK-571 (sodium salt) can be prepared by directly dissolving the crystalline compound in aqueous buffers. The solubility of MK-571 (sodium salt) in PBS (pH 7.2) is approximately 10 mg/ml. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Lynch, K.R., O’Neill, G.P., Liu, Q., et al. Nature 399, 789-793 (1999).
  2. Heise, C.E., O’Dowd, B.F., Figueroa, D.J., et al. J. Biol. Chem. 275, 30531-30536 (2000).
  3. Jones, T.R., Zamboni, R., Belley, M., et al. Can. J. Physiol. Pharmacol. 67, 17-28 (1989).
  4. Ogasawara, H., Ishii, S., Yokomizo, T., et al. J. Biol. Chem. 277(21), 18763-18768 (2002).
  5. Dallas, S., Zhu, X., Baruchel, S., et al. J. Pharmacol. Exp. Ther. 307(1), 282-290 (2003).

 


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