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Vipoglanstat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vipoglanstat图片
CAS NO:1360622-01-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议

产品名称
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[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].

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.
Clinical Trial
分子量

678.52

性状

Solid

Formula

C30H34Cl2F5N5O3

CAS 号

1360622-01-0

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.4738 mL7.3690 mL14.7380 mL
5 mM0.2948 mL1.4738 mL2.9476 mL
10 mM0.1474 mL0.7369 mL1.4738 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。