Verlukast

Verlukast, also known as MK-0679, is a (R)-enantiomer of MK-571 and a potent and selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig (IC50 = 3.1 +/- 0.5 nM) and human (IC50 = 8.0 +/- 3.0 nM) lung homogenates and dimethyl sulfoxide differentiated U937 cell membrane preparations (IC50 = 10.7 +/- 1.6 nM) but is essentially inactive versus [3H]leukotriene C4 binding in guinea-pig lung homogenates (IC50 values of 19 and 33 microM). Verlukast was in clinical development for the treatment of asthma and related diseases. (last updated: 8/8/2016)

Product information

CAS Number: 120443-16-5

Molecular Weight: 515.09

Formula: C26H27ClN2O3S2

Synonym:

MK-679

L 668019

MK-0679

MK0679

L668019

L-668019

Chemical Name: 3-{[(R)-{3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl}({[2-(dimethylcarbamoyl)ethyl]sulfanyl})methyl]sulfanyl}propanoic acid

Smiles: CN(C)C(=O)CCS[C@H](SCCC(O)=O)C1=CC(/C=C/C2=CC=C3C=CC(Cl)=CC3=N2)=CC=C1

InChiKey: AXUZQJFHDNNPFG-LHAVAQOQSA-N

InChi: InChI=1S/C26H27ClN2O3S2/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)/b10-6+/t26-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Hsieh JY, Lin C, Matuszewski BK. Robotic sample preparation and high-performance liquid chromatographic analysis of verlukast in human plasma. J Chromatogr B Biomed Appl. 1994 Nov 18;661(2):307-12.
2. Schwartz JI, Margolskee DJ, Bjornsson TD, Williams VC, Hsieh JY, Lin CC, Rogers JD. Oral pharmacokinetics and food interaction of the leukotriene D4 receptor antagonist verlukast. Br J Clin Pharmacol. 1993 Nov;36(5):464-6.

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