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 引发浓度依赖性抑制 LTB₄ 诱导的 CD11b 上调^[1]。
Etalocib sodium 是一种体外极其有效且选择性的人类中性粒细胞功能拮抗剂^[2]。
Etalocib (250 和 500 nM, 24-72 小时) sodium 诱导人胰腺癌细胞凋亡并抑制其增殖^[3]。

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

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

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

566.59

C₃₃H₃₂FNaO₆

152608-41-8

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]