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Gemilukast

CAS No. : 1232861-58-3

MCE 站：Gemilukast

产品活性：Gemilukast 是具有口服活性的、有效的半胱氨酰白三烯 1 和 2 受体 (CysLT₁ 和CysLT₂) 的双抑制剂，其对人 CysLT₁ 和 CysLT₂ 的 IC₅₀ 值分别为 1.7 nM 和 25 nM。

研究领域：GPCR/G Protein

作用靶点：Leukotriene Receptor

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. Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT₁ receptor-mediated calcium response with IC₅₀ values of 1.7 and 0.46 nM, respectively.

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.

相关产品：Orally Active Compound Library  |  GPCR/G Protein Compound Library  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Montelukast sodium  |  MK-571 sodium salt  |  MK-886  |  Zafirlukast  |  Pranlukast  |  Fiboflapon  |  Nedocromil  |  LY223982  |  11-?Keto-?beta-?boswellic acid  |  AS-35  |  BIIL-260 hydrochloride  |  Darbufelone  |  Veliflapon  |  (S)-Verapamil hydrochloride  |  5-O-Demethylnobiletin  |  CP-96021 hydrochloride  |  HAMI 3379  |  LM-1484  |  Quinotolast sodium  |  RG-12525  |  RS-601  |  Tipelukast  |  Amelubant  |  Bunaprolast  |  CI-949  |  CP-105696

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