1. GPCR/G Protein
  2. Leukotriene Receptor
  3. Gemilukast

Gemilukast (Synonyms: ONO-6950)

Cat. No.: HY-16780
Handling Instructions

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.

For research use only. We do not sell to patients.

Gemilukast Chemical Structure

Gemilukast Chemical Structure

CAS No. : 1232861-58-3

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Description

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.

IC50 & Target[1]

CysLT1

1.7 nM (IC50, in human)

CysLT2

25 nM (IC50, in human)

In Vitro

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively[1]. Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT1 receptor-mediated calcium response with IC50 values of 1.7 and 0.46 nM, respectively[2].

In Vivo

Gemilukast at 0.03 to 10 mg/kg, p.o. dose-dependently attenuates LTC4-induced bronchoconstriction with almost complete inhibition at 3 mg/kg. The inhibitory effect of Gemilukast on LTC4-induced bronchoconstriction is significantly stronger than that of montelukast at the dose of 1 mg/kg or more. Gemilukast (0.03 to 1 mg/kg, p.o.) dose-dependently attenuates LTD4-induced airway vascular hyperpermeability with complete inhibition at 0.3 mg/kg. Gemilukast at 0.1 to 3 mg/kg, p.o. dose-dependently inhibits OVA-induced bronchoconstriction. The inhibitory effect of Gemilukast at 3 mg/kg is significantly greater than that of montelukast alone and comparable to that of combination therapy with montelukast and BayCysLT2RA[2].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vivo:
  • 1.

    ONO-6950 is suspended in 0.5 w/v% methylcellulose solution[2].

References
Molecular Weight

601.68

Formula

C₃₆H₃₇F₂NO₅

CAS No.

1232861-58-3

SMILES

O=C(O)CCCN1C(C)=C(CCCC(O)=O)C2=C1C(C#CC3=CC=C(OCCCCC4=CC=CC(F)=C4C)C=C3)=CC=C2F

Shipping

Room temperature in continental US; may vary elsewhere

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Gemilukast
Cat. No.:
HY-16780
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Gemilukast

Cat. No.: HY-16780