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。

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT 1 and CysLT 2 ) antagonist, with IC 50 s of 1.7, 25 nM for human CysLT 1 and CysLT 2 , respectively.

Solid

CysLT1 1.7 nM (IC50, in human) CysLT2

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Itadani S, et al. Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma. J Med Chem. 2015 Aug 13;58(15):6093-113.
[2]. Yonetomi Y, et al. Effects of ONO-6950, a novel dual cysteinyl leukotriene 1 and 2 receptors antagonist, in a guinea pig model of asthma. Eur J Pharmacol. 2015 Oct 15;765:242-8.

In Vitro: DMSO : 250 mg/mL (415.50 mM; Need ultrasonic)配制储备液