1. GPCR/G Protein
    Apoptosis
  2. Leukotriene Receptor
    Apoptosis
  3. Etalocib

Etalocib (Synonyms: LY293111; VML 295)

Cat. No.: HY-13628
Handling Instructions

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.

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Etalocib Chemical Structure

Etalocib Chemical Structure

CAS No. : 161172-51-6

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Description

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[1][2][3].

In Vitro

Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB4 induced CD11b up-regulation[1].
Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro[2].
Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells[3].

Cell Proliferation Assay[3]

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[3]

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.
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)[2].
Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h[2].
Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice[3].

Animal Model: Guinea pigs[2].
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.
Molecular Weight

544.61

Formula

C₃₃H₃₃FO₆

CAS No.

161172-51-6

SMILES

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EtalocibLY293111VML 295LY 293111LY-293111VML295VML-295Leukotriene ReceptorApoptosisPulmonaryantiinflammatoryasthmabronchiectasisInhibitorinhibitorinhibit

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