Vipoglanstat (BI 1029539),甲酰胺,是一种有效的,选择性的,非肽人前列腺素 E 合成酶 1(mPGES-1)小分子抑制剂,具有口服活性。Vipoglanstat 也具有抗炎活性。
生物活性 | Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1(mPGES-1). Vipoglanstat also has anti-inflammatory activity[1][2]. |
体外研究 (In Vitro) | Vipoglanstat significantly inhibits mPGES-1 level (IC50: about 1 nM)[3]. Vipoglanstat blocks the up-regulation of P-gp and mPGES-1 levels on glutamate-mediatedin isolated brain capillaries[3]. Vipoglanstat reduces human peripheral blood inflammatory cell migration and inflammatory mediator release[3].
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体内研究 (In Vivo) | Vipoglanstat (30 mg/kg; i.p.) can reduce LPS-induced lung injury, with reduction in neutrophil influx, protein content, TNF-ɑ, IL-1β and PGE2 levels in bronchoalveolar lavage (BAL), myeloperoxidase activity, expression of mPGES-1, cyclooxygenase (COX)-2 and intracellular adhesion molecule in lung tissue[2]. Vipoglanstat (30 mg/kg; p.o.; 2 h, 8 h and 22 h) significantly reduces sepsis-induced BAL inflammatory cell recruitment, lung injury score and lung expression of mPGES-1 and inducible nitric oxide synthase[2]. Vipoglanstat (30 mg/kg; p.o.; QD) also significantly prolongs survival of mice with severe sepsis[2].
Animal Model: | LPS-induced acute lung injury models[2] | Dosage: | 30 mg/kg | Administration: | 30 mg/kg, i.p. | Result: | Preserved lung architecture and reduced immune cell influx into the lungs of LPS-challenged mice. |
Animal Model: | CLP-induced sepsis models[2] | Dosage: | 30 mg/kg | Administration: | 30 mg/kg, p.o., 2 hrs, 8 hrs and 22 hrs; 30 mg/kg, p.o., QD | Result: | Attenuated CLP-induced lung injury and prolongs survival. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 150 mg/mL(221.07 mM;Need ultrasonic) 配制储备液 1 mM | 1.4738 mL | 7.3690 mL | 14.7380 mL | 5 mM | 0.2948 mL | 1.4738 mL | 2.9476 mL | 10 mM | 0.1474 mL | 0.7369 mL | 1.4738 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 (sealed storage, away from moisture and light)。-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%corn oil Solubility: ≥ 3.75 mg/mL (5.53 mM); Clear solution
此方案可获得 ≥ 3.75 mg/mL (5.53 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 37.5 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。 |