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128312-51-6

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128312-51-6 Structure

128312-51-6 Structure
IdentificationBack Directory
[Name]

CINALUKAST
[CAS]

128312-51-6
[Synonyms]

Ro 24-591
CINALUKAST
RO 24-5913
C·Nalukast
2,2-Diethyl-N-[3-[(E)-2-(4-cyclobutyl-2-thiazolyl)ethenyl]phenyl]succinamidic acid
(E)-4-[[3-(2-(4-CYCLOBUTYL-2-THIAZOLYL)ETHENYL)PHENYL]AMINO]-2,2-DIETHYL-4-OXOBUTANOIC ACID
4-[[3-[(1E)-2-(4-CYCLOBUTYL-2-THIAZOLYL)ETHENYL]PHENYL]AMINO]-2,2-DIETHYL-4-OXOBUTANOIC ACID
Butanoic acid, 4-[[3-[(1E)-2-(4-cyclobutyl-2-thiazolyl)ethenyl]phenyl]aMino]-2,2-diethyl-4-oxo-
Ro 24-5913, (E)-4-[[3-(2-(4-Cyclobutyl-2-thiazolyl)ethenyl)phenyl]amino]-2,2-diethyl-4-oxobutanoic acid
[Molecular Formula]

C23H28N2O3S
[MDL Number]

MFCD00864778
[MOL File]

128312-51-6.mol
[Molecular Weight]

412.55
Chemical PropertiesBack Directory
[storage temp. ]

2-8°C
[solubility ]

DMSO: >10 mg/mL
[form ]

Powder
[color ]

off-white
Safety DataBack Directory
[Safety Statements ]

22-24/25
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

A novel leukotriene D4 antagonist
[Uses]

A novel leukotriene D4 antagonist.
[Definition]

ChEBI: 2,2-Diethylsuccinanilic acid substituted at a meta- position by an (E)-2-(4-cyclobutyl-1,3-thiazol-2-yl)ethenyl group. It selectively antagonizes leukotriene D4 at the cysteinyl leukotriene receptor, in th human airway, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus. It is used in the treatment of asthma.
[Biological Activity]

Potent, selective CysLT 1 (LTD 4 ) leukotriene receptor antagonist (IC 50 = 6.4 nM). Inhibits LTD 4 -induced bronchoconstriction in guinea pigs when administered intravenously, orally or by aerosol.
[in vivo]

Ro 24-5913 (10 mg/kg i.v. and 100 mg/kg p.o.; once) inhibits LTD4-induced bronchoconstriction in guinea pigs with LD50s of 0.13 and 0.12 mg/kg for i.v. and p.o. respectively[1].

Animal Model:Guinea pigs[1]
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once
Result:Inhibited LTD4-induced bronchoconstnction and antigen-induced bronchoconstnction in guinea pigs.
[storage]

Desiccate at -20°C
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