Etalocib

生物活性体外研究体内研究 Etalocib 试剂级价格

Etalocib

CAS号:161172-51-6
英文名:Etalocib
中文名:Etalocib
CBNumber:CB61856046
分子式:C33H33FO6
分子量:544.61
MOL File:161172-51-6.mol

Etalocib化学性质

熔点 :68-70 °C(Solv: acetonitrile (75-05-8))
沸点 :656.8±55.0 °C(Predicted)
密度 :1?+-.0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO:98.5(Max Conc. mg/mL);173.85(Max Conc. mM)
形态 :Solid
酸度系数(pKa) :3.32±0.36(Predicted)
颜色 :White to off-white

Etalocib性质、用途与生产工艺

生物活性 Etalocib (LY293111) 是具有口服活性的白三烯 (LTB4) 受体的拮抗剂，抑制 [3H]LTB4 结合的Ki 值为 25 nM. Etalocib (LY293111) 抑制LTB4 诱导的钙动员的 lC50 值为 20 nM。Etalocib (LY293111) 可诱导凋亡。

体外研究

Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB ₄ 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.

Cell Proliferation Assay

Cell Line:	MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. ^[3]
Concentration:	500 nM.
Incubation Time:	24, 48, and 72 h.
Result:	Caused both a concentration-dependent and time-dependent inhibition of thymidine incorporation in both MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.

Apoptosis Analysis

Cell Line:	MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.
Concentration:	250 and 500 nM.
Incubation Time:	24 h.
Result:	Induced apoptosis in human pancreatic cancer cells.

体内研究

Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B ₄ -induced airway obstruction when administered i.v. (ED ₅₀ =14 µg/kg) or p.o. (ED ₅₀ =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 B ₄ 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.