Etalocib

Research use only, not for human use.

Etalocib is a novel diaryl ether carboxylic acid derivative, is a selective and potent inhibitor of the lipoxygenase pathway either via antagonism of the leukotriene B4 (LTB4) receptor or directly through 5'-lipoxygenase.

Etalocib is a novel diaryl ether carboxylic acid derivative, is a selective and potent inhibitor of the lipoxygenase pathway either via antagonism of the leukotriene B4 (LTB4) receptor or directly through 5'-lipoxygenase. It has antineoplastic activities.(In Vitro):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.(In Vivo):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.

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. Cell Proliferation Assay Cell Line:MiaPaCa-2 and AsPC-1 human pancreatic cancer cells. 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.

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.

LY293111 | VML295

Apoptosis

Apoptosis

Apoptosis|LTB4

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161172-51-6

544.6

C33H33FO6

>98% (HPLC)

DMSO:100 mg/mL (183.62 mM; Need ultrasonic)

O=C(O)C1=CC=CC=C1OC2=CC=CC(OCCCOC3=C(CC)C=C(C4=CC=C(F)C=C4)C(O)=C3)=C2CCC

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(-20℃)

With Ice Pack

≥ 2 years