Etalocib LY293111; VML 295|cas:161172-51-6|西域试剂

Etalocib LY293111; VML 295,98.27%

产品编号：Bellancom-13628| CAS NO：161172-51-6| 分子式：C₃₃H₃₃FO₆| 分子量：544.61

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-13628	￥4200.00	杭州北京（现货）
Bellancom-13628	￥6800.00	杭州北京（现货）
Bellancom-13628	￥13500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Etalocib 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K_i 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 active leukotriene B₄ receptor antagonist, inhibits the binding of [³H]LTB₄, with a K_i of 25 nM. Etalocib (LY293111) prevents LTB₄-induced calcium mobilization with an lC₅₀ of 20 nM. Etalocib (LY293111) induces apoptosis.

体外研究

Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB₄ 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.

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

Cell Proliferation Assay

Cell Line:	MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.
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
(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).
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.

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

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 B₄ 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.

体内研究

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

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 B₄ 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.

体内研究

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

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 B₄ 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.

性状

Solid

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 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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 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。