Varespladib (LY315920) 是一种有效且具有选择性的group IIA, secretory phospholipase A2(sPLA2)抑制剂，其IC50值为 9 nM。Varespladib 对大鼠，兔，豚鼠和人等各种物种血清的sPLA2活性具有明显的抑制作用，IC50分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。
| 生物活性 | Varespladib (LY315920) is a potent and selectivegroup IIA, secretoryphospholipase A2(sPLA2)inhibitor with anIC50of 9 nM. Varespladib exhibits the significant inhibitory effect onsPLA2activity in serum from various species including rat, rabbit, guinea pig and human withIC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1]. |
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体外研究
(In Vitro) | Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points[2].
Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours[2].
Western Blot Analysis[2] | Cell Line: | HCjE cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours and 48 hours | | Result: | Significantly inhibited the RA-induced MUC16 protein expression at both time points. |
RT-PCR[2] | Cell Line: | HCjE cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours and 48 hours | | Result: | Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours. |
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体内研究
(In Vivo) | Varespladib treatment inhibits human sPLA2-induced release of thromboxane A2(TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with anIC50of 0.79 μM. And theED50for Varespladib is 16.1 mg/kg[1].
| Animal Model: | Male Hartley guinea pigs (300-500 g)[1] | | Dosage: | 3 mg/kg, 10 mg/kg, and 30 mg/kg | | Administration: | Intravenous injection (Pharmacokinetic study) | | Result: | Consistent inhibition of sPLA2activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2on BAL cells from guinea pigs. |
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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(262.89 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 2.6289 mL | 13.1444 mL | 26.2888 mL | | 5 mM | 0.5258 mL | 2.6289 mL | 5.2578 mL | | 10 mM | 0.2629 mL | 1.3144 mL | 2.6289 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 (6.57 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.57 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： 17% Polyethylene glycol 12-hydroxystearate in saline Solubility: 1.5 mg/mL (3.94 mM); Suspended solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
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