产品
编 号：F193182
分子式：C33H33FO6
分子量：544.61
分子式：C33H33FO6
分子量：544.61
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 161172-51-6
产品详情
生物活性：
Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
体内研究：
Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B4-induced airway obstruction when administered i.v. (ED50=14 μg/kg) or p.o. (ED50=0.4 mg/kg).Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h.Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice.Animal Model:Guinea pigs.
Dosage:1-10 mg/kg.
Administration:Orally once.
Result:A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B4 challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge.Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge.
体外研究：
Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB4 induced CD11b up-regulation.Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro.Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells.
Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
体内研究：
Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B4-induced airway obstruction when administered i.v. (ED50=14 μg/kg) or p.o. (ED50=0.4 mg/kg).Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h.Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice.Animal Model:Guinea pigs.
Dosage:1-10 mg/kg.
Administration:Orally once.
Result:A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B4 challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge.Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge.
体外研究：
Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB4 induced CD11b up-regulation.Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro.Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells.
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