GW627368 (GW627368X) 是前列腺素受体EP4高效选择竞争性抑制剂,还对血栓素受体TP有亲和力。对人 EP4 和 TP 的pKi值分别为 7.0 和 6.8。
生物活性 | GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoidEP4receptor with additional humanTPreceptor affinity, withpKivalues of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively[1]. |
IC50& Target | pKi :7.0 (hEP4), 6.8 (hTP)[1] |
体外研究 (In Vitro) | GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species[1]. GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets[1]. GW627368 (GW627368X) is devoid of agonist activity and actually produced a significant and concentration-related reduction in basal cAMP levels with pIC50value of 6.3[1]. GW627368 (GW627368X) induces inhibition of proliferation and invasion of human SUM149 IBC tumor cells beginning at 0.1 μM, with inhibition of proliferation and invasion of MDA-MB-231 non-IBC cells at higher concentrations[2].
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体内研究 (In Vivo) | GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis[3].
Animal Model: | 6-8 weeks Swiss albino mice[3] | Dosage: | 0 mg/kg, 5 mg/kg, 10 mg/kg, 15 mg/kg, 15 mg/kg | Administration: | Oral administration, every alternate day for 28 days | Result: | Displayed anti-tumor and anti-proliferative potential in sarcoma 180 bearing mice. |
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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 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(183.61 mM;Need ultrasonic) 配制储备液 1 mM | 1.8361 mL | 9.1807 mL | 18.3614 mL | 5 mM | 0.3672 mL | 1.8361 mL | 3.6723 mL | 10 mM | 0.1836 mL | 0.9181 mL | 1.8361 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 40%PEG300 5%Tween-80 45% saline 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。 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%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。
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