Vipoglanstat
(Synonyms: BI 1029539; GS-248; OX-MPI) 目录号 : GC70119Vipoglanstat (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。
Cas No.:1360622-01-0
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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. |
[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 therapeutic significance. Pharmacol Res. 2022 Jan;175:105977.
| Cas No. | 1360622-01-0 | SDF | Download SDF |
| 别名 | BI 1029539; GS-248; OX-MPI | ||
| 分子式 | C30H34Cl2F5N5O3 | 分子量 | 678.52 |
| 溶解度 | DMSO : 150 mg/mL (221.07 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4738 mL | 7.369 mL | 14.738 mL |
| 5 mM | 0.2948 mL | 1.4738 mL | 2.9476 mL |
| 10 mM | 0.1474 mL | 0.7369 mL | 1.4738 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet