Etalocib sodium  (Synonyms: LY293111 sodium; VML 295 sodium)

Etalocib (LY293111) sodium, an orally active leukotriene B₄ receptor antagonist, inhibits the binding of [³H]LTB₄, with a K_i of 25 nM. Etalocib sodium prevents LTB₄-induced calcium mobilization with an lC₅₀ of 20 nM. Etalocib sodium induces apoptosis^[1][2][3].

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

566.59

C₃₃H₃₂FNaO₆

152608-41-8

O=C(C1=C(OC2=CC=CC(OCCCOC3=C(CC)C=C(C4=CC=C(F)C=C4)C(O)=C3)=C2CCC)C=CC=C1)O[Na]

Room temperature in continental US; may vary elsewhere.

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

• [1]. P Marder, et al. Blockade of Human Neutrophil Activation by 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- Hydroxyphenoxy]propoxy]phenoxy]benzoic Acid (LY293111), a Novel Leukotriene B4 Receptor Antagonist. Biochem Pharmacol. 1995 May 26;49(11):1683-90.  [Content Brief]

  [2]. S A Silbaugh, et al. Pharmacologic Actions of the Second Generation Leukotriene B4 Receptor Antagonist LY29311: In Vivo Pulmonary Studies. Naunyn Schmiedebergs Arch Pharmacol. 2000 Apr;361(4):397-404.  [Content Brief]

  [3]. Wei-Gang Tong, et al. Leukotriene B4 Receptor Antagonist LY293111 Inhibits Proliferation and Induces Apoptosis in Human Pancreatic Cancer Cells. Clin Cancer Res. 2002 Oct;8(10):3232-42.  [Content Brief]