Etalocib
- CAS号:161172-51-6
- 英文名:Etalocib
- 中文名:Etalocib
- CBNumber:CB61856046
- 分子式:C33H33FO6
- 分子量:544.61
- MOL File:161172-51-6.mol
- 熔点 :68-70 °C(Solv: acetonitrile (75-05-8))
- 沸点 :656.8±55.0 °C(Predicted)
- 密度 :1?+-.0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:98.5(Max Conc. mg/mL);173.85(Max Conc. mM)
- 形态 :Solid
- 酸度系数(pKa) :3.32±0.36(Predicted)
- 颜色 :White to off-white
Etalocib性质、用途与生产工艺
- 生物活性 Etalocib (LY293111) 是具有口服活性的白三烯 (LTB4) 受体的拮抗剂，抑制 [3H]LTB4 结合的Ki 值为 25 nM. Etalocib (LY293111) 抑制LTB4 诱导的钙动员的 lC50 值为 20 nM。Etalocib (LY293111) 可诱导凋亡。
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体外研究
Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB 4 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. [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
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. -
体内研究
Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B 4 -induced airway obstruction when administered i.v. (ED 50 =14 µg/kg) or p.o. (ED 50 =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 B 4 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.
- 更新日期：2024/11/08
- 产品编号：HY-13628
- 产品名称：Etalocib
- CAS编号：
- 包装：1 mg
- 价格：1500元
- 更新日期：2024/11/08
- 产品编号：HY-13628
- 产品名称：Etalocib Etalocib
- CAS编号：161172-51-6
- 包装：5mg
- 价格：3300元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：32161
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57505
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- 公司名称：CAYMAN
- 联系电话：--
- 电子邮件：cayman@caymanchem.com
- 国家：美国
- 产品数：6213
- 优势度：81
- 公司名称：United States Biological Inc.
- 联系电话：--
- 电子邮件：chemicals@usbio.net
- 国家：美国
- 产品数：6214
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- 公司名称：MedChemExpress
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- 国家：美国
- 产品数：6398
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