产品说明书

Taprenepag

Print
Chemical Structure| 752187-80-7 同义名 : CP-544326;CP 544,326;CP544326, CP544326, Taprenepag, PF-0421732 metabolite
CAS号 : 752187-80-7
货号 : A152959
分子式 : C24H22N4O5S
纯度 : 99%+
分子量 : 478.52
MDL号 : MFCD18633300
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(219.43 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.04mL

20.90mL

4.18mL

2.09mL
参考文献

[1]Yanochko GM, Affolter T, et al. Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma. J Ocul Pharmacol Ther. 2014 Jun;30(5):429-39.

[2]Prasanna G, Carreiro S, et al. Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure inpreclinical models of glaucoma. Exp Eye Res. 2011 Sep;93(3):256-64.

[3]Kristy E Gilman,et al. The complex role of prostaglandin E 2-EP receptor signaling in wound healing. Am J Physiol Regul Integr Comp Physiol. 2021. 320(3), R287-R296.

[4]Jocelyn Reader,et al. Prostaglandin E2 EP receptors as therapeutic targets in breast cancer. Cancer Metastasis Rev. 2011. 30(3-4), 449-63.

[5]Prasanna G, et al. Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure inpreclinical models of glaucoma. Exp Eye Res. 2011. 93(3), 256-64.