|2-(3-(3-((5-乙基-4'-氟-2-羟基-[1,1'-联苯]-4-基)氧基)丙氧基)-2-丙基苯氧基)苯甲酸|CsnPharm

CAS No.: 161172-51-6

Etalocib Catalog No. CSN28763

Synonyms: LY293111;VML 295;PDSP1001237

LY293111 is a potent LTB4 receptor antagonist with IC50 values of 17.6nM and 6.3nM for inhibition of the specific binding of radiolabeled-LTB4 to isolated human neutrophils and the LTB4-induced chemotaxis of human neutrophils, respectively.

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技术信息

生物活性

描述Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. LY293111 prevented LTB4-induced calcium mobilization with an IC50 = 20 nM, or 40 times more effectively than SC-41930 (IC50 = 808 nM). LY293111 was 300 times more potent than SC-41930 in blocking LTB4-induced CD11b up-regulation on isolated neutrophils. LY293111 also arrested LTB4-induced up-regulation of CD11b on neutrophils in whole human blood. LY293111 was not effective in blocking human neutrophil activation responses induced by N-formyl-methionyl-leucyl-phenylalanine (fMLP), platelet-activating factor (PAF), human recombinant endothelial interleukin-8 (IL-8) or human recombinant complement component 5a (C5a).^[2]. LY293111 sodium produced a dose-related inhibition of acute leukotriene B4-induced airway obstruction when administered i.v. (ED50=14 microg/kg) or p.o. (ED50=0.4 mg/kg). In contrast, LY293111 sodium did not inhibit the pulmonary gas trapping caused by aerosols of histamine, leukotriene D4, or the thromboxane mimetic U46619. Oral LY293111 sodium inhibited leukotriene B4-induced bronchoalveolar lavage granulocyte infiltration and delayed onset airway obstruction at doses as low as 0.3 mg/kg. In A23187-challenged animals, pulmonary inflammation was markedly inhibited at 1 h, but not 2 h and 4 h post-exposure. LY293111 sodium is a selective leukotriene B4 receptor antagonist with potent pulmonary anti-inflammatory activity^[3].The LTB4 receptor antagonist LY293111 caused both time- and concentration-dependent inhibition of proliferation of all six human pancreatic cancer cell lines studied. LY293111 induced apoptosis in these pancreatic cancer cell lines, as indicated by morphology, TUNEL assay, and poly(ADP-ribose) polymerase cleavage.Using AsPC-1 and HPAC cell xenografts in athymic mice, LY293111 treatment markedly inhibited tumor growth over a 24-day treatment period, as measured by both tumor volume and tumor weight. In situ tissue TUNEL assay showed massive apoptosis in LY293111-treated tumor tissues^[4].
参考文献

[1] Jackson WT, Froelich LL, Boyd RJ, Schrementi JP, Saussy DL Jr, Schultz RM, Sawyer JS, Sofia MJ, Herron DK, Goodson T Jr, Snyder DW, Pechous PA, Spaethe SM, Roman CR, Fleisch JH. Pharmacologic actions of the second-generation leukotriene B4 receptor antagonist LY293111: in vitro studies. J Pharmacol Exp Ther. 1999 Jan;288(1):286-94. PMID: 9862783.
[2] 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.
[3] 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.
[4] 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8362 mL
- 9.1809 mL
- 18.3618 mL
- 5 mM
- 0.3672 mL
- 1.8362 mL
- 3.6724 mL
- 10 mM
- 0.1836 mL
- 0.9181 mL
- 1.8362 mL

技术信息

CAS号	161172-51-6	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C33H33FO6	运输	蓝冰
分子量	544.61	别名	LY293111;VML 295;PDSP1001237;PDSP2001221

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