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。
| 生物活性 | Etalocib (LY293111), an orally activeleukotriene B4receptorantagonist, inhibits the binding of[3H]LTB4, with aKiof 25 nM. Etalocib (LY293111) preventsLTB4-induced calcium mobilization with anlC50of 20 nM. Etalocib (LY293111) inducesapoptosis[1][2][3]. |
体外研究
(In Vitro) | Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB4induced 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. |
|
体内研究
(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 B4challenge, 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.
|
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(183.62 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.59 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.59 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.59 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
m.cnreagent.com