Vipoglanstat (Synonyms: BI 1029539; GS-248; OX-MPI)
目录号: PL09522 纯度: ≥99%
CAS No. :1360622-01-0
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中文名称
Vipoglanstat
英文名称
Vipoglanstat
英文别名
1H-Benzimidazole-5-carboxamide, 2-[[2,6-dichloro-3-[[(2,2-dimethyl-1-oxopropyl)amino]methyl]phenyl]amino]-6-(2,2-difluoroethoxy)-1-methyl-N-[trans-4-(trifluoromethyl)cyclohexyl]-;Vipoglanstat
Cas No.
1360622-01-0
分子式
C30H34Cl2F5N5O3
分子量
678.52
包装储存
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)
产品详情
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.
性状
Solid
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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)
ClinicalTrial
参考文献
[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022.
[2]. Malarvizhi Gurusamy, et al. Inhibition of microsomal prostaglandin E synthase-1 ameliorates acute lung injury in mice.
[3]. Yan-Yu Zhang, et al. Microsomal prostaglandin E 2 synthase-1 and its inhibitors: Molecular mechanisms and the
溶解度数据
In Vitro: DMSO : 150 mg/mL (221.07 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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