752187-80-7|Taprenepag|CsnPharm

CAS No.: 752187-80-7

Taprenepag Catalog No. CSN18419

Synonyms: CP-544326;CP 544,326;PF-0421732 metabolite

Taprenepag is an agonist of prostaglandin E2 receptor with EC50 of 2.8 nM with hypotensive activity.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Prostaglandin EP2 Receptor

EC50:2.8nM
描述Prostaglandins are critical lipid mediators involved in the wound healing response, with prostaglandin E2 (PGE2) being the most complex and exhibiting the most diverse physiological outputs.^[3]. Prostaglandin E2 (PGE(2)) is the most abundant prostanoid in the human body, and synthesis of PGE(2) is driven by cyclooxygenase enzymes including COX-2. Both elevated expression of COX-2 and increased PGE(2) levels have been associated with many cancers including breast cancer^[4]. Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors. Taprenepag (CP-544326) (0.01-1000 nM) increases cAMP levels in HEK293 cells expressing human EP2 (EC50=2.8 nM). CP-544326 was found to be a potent and selective EP(2) agonist (IC(50) = 10 nM; EC(50) = 2.8 nM) whose corneal permeability and ocular bioavailability were significantly increased when the compound was dosed as the isopropyl ester prodrug, PF-04217329^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0898 mL
- 10.4489 mL
- 20.8978 mL
- 5 mM
- 0.4180 mL
- 2.0898 mL
- 4.1796 mL
- 10 mM
- 0.2090 mL
- 1.0449 mL
- 2.0898 mL

技术信息

CAS号

752187-80-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H22N4O5S

运输

蓝冰

分子量

478.52

别名

CP-544326;CP 544,326;PF-0421732 metabolite

溶解度

DMSO	98.0 mg/mL (204.8 mM)

动物实验配方

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Taprenepag Catalog No. CSN18419

靶点选择性

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