Vipoglanstat BI 1029539; GS-248; OX-MPI|cas:1360622-01-0|西域试剂

Vipoglanstat BI 1029539; GS-248; OX-MPI,99.74%

产品编号：Bellancom-147416| CAS NO：1360622-01-0| 分子式：C₃₀H₃₄Cl₂F₅N₅O₃| 分子量：678.52

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-147416		￥5800.00	杭州北京（现货）

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Vipoglanstat BI 1029539; GS-248; OX-MPI

产品介绍

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.

体外研究

Vipoglanstat significantly inhibits mPGES-1 level (IC₅₀: about 1 nM).
Vipoglanstat blocks the up-regulation of P-gp and mPGES-1 levels on glutamate-mediatedin isolated brain capillaries.
Vipoglanstat reduces human peripheral blood inflammatory cell migration and inflammatory mediator release.

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

体内研究

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.
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.
Vipoglanstat (30 mg/kg; p.o.; QD) also significantly prolongs survival of mice with severe sepsis.

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

Animal Model:	LPS-induced acute lung injury models
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
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.

体内研究

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

Animal Model:	LPS-induced acute lung injury models
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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 150 mg/mL (221.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4738 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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% 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。