LY255283
目录号 : KM7508 CAS No. : 117690-79-6 纯度 : 98%

LY255283 是 LTB4 受体 (BLT2) 的拮抗剂,其抑制 [3H]LTB4 结合到豚鼠肺膜的 IC50 值约为 100 nM。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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25mg
In-stock
50mg
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100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [H]LTB4 binding to guinea pig lung membranes.

体外研究

LY255283 competitively reduces conlractilc responses of lung parcnchyma to LTB, (pA2 = 7.2).
LY255283 (10 μM, 7 days) significantly suppresses the invasiveness of highly aggressive 253 J-BV bladder cancer cells.

Cell Viability Assay

Cell Line: 253 J-BV cells.
Concentration: 5 or 10 μM.
Incubation Time: 7 days.
Result: Inhibition of BLT2 signaling attenuates aggressive migration by 253 J-BV cells.
体内研究

LY255283 (3, 30 mg/kg) ameliorates lipopolysaccharide-induced ARDS in pigs, possibly by blocking the recruitment of activated PMNs into alveoli in a dose-dependent fashion.
LY255283 (2.5 mg/kg, ip) inhibits transitional cell carcinoma metastasis in mice models. The result suggests that a BLT2–Nox–ROS–NF–κB cascade plays a critical role in bladder cancer invasion and metastasis.

Animal Model: Mice (253 J-BV cells injected).
Dosage: 2.5 mg/kg.
Administration: IP injected 3 and 5 days after injection of cells.
Result: By 12 weeks after injection, in mice treated with LY255283 only 0-3 nodules formed per lung, and histological analysis confirmed that the number of micrometastatic lesions was markedly reduced.
分子式
C19H28N4O3
分子量
360.45
CAS号
117690-79-6
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (277.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7743 mL 13.8715 mL 27.7431 mL
5 mM 0.5549 mL 2.7743 mL 5.5486 mL
10 mM 0.2774 mL 1.3872 mL 2.7743 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 (stored under nitrogen)。-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    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.94 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.94 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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.94 mM,饱和度未知) 的澄清溶液。

    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。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.94 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。

科研文献
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