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Etalocib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Etalocib图片
CAS NO:161172-51-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
LY293111
VML 295
产品介绍
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

544.61

性状

Solid

Formula

C33H33FO6

CAS 号

161172-51-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(183.62 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8362 mL9.1809 mL18.3618 mL
5 mM0.3672 mL1.8362 mL3.6724 mL
10 mM0.1836 mL0.9181 mL1.8362 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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。