1201925-19-0
Chemical Structure
PF-04475270
- CAS No.: 1201925-19-0
- Formula:C26H32F3NO4S
- Molecular Weight:511.60
InChIKey: SCEAAZFMDOEZAH-LEWJYISDSA-N
SMILES: FC(F)(F)C1=CC=CC(C[C@H](O)CC[C@@H]2N(C(CC2)=O)CCCC3=CC=C(C(OC(C)C)=O)S3)=C1
Biological Activity: PF-04475270 is a prodrug of CP-734432 (HY-119236), as well as an agonist of the EP4 prostaglandin receptor, with IC50 values of 2 nM and 8 nM against human and canine sources, respectively. PF-04475270 is rapidly hydrolyzed into its active metabolite CP-734432 by ocular esterases or corneal homogenate, stimulates cAMP production, and activates cAMP response element-mediated β-lactamase activity in cells expressing EP4. PF-04475270 can be used in research related to glaucoma[1][2].
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PF-04475270 | PF-04475270 is a prodrug of CP-734432 (HY-119236), as well as an agonist of the EP4 prostaglandin receptor, with IC50 values of 2 nM and 8 nM against human and canine sources, respectively. PF-04475270 is rapidly hydrolyzed into its active metabolite CP-734432 by ocular esterases or corneal homogenate, stimulates cAMP production, and activates cAMP response element-mediated β-lactamase activity in cells expressing EP4. PF-04475270 can be used in research related to glaucoma. | |||||||||||||||||||||
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- [1]. Luu KT, et al. Pharmacokinetic-pharmacodynamic and response sensitization modeling of the intraocular pressure-lowering effect of the EP4 Agonist 5-{3-[(2S)-2-{(3R)-3-hydroxy-4-[3-(trifluoromethyl)phenyl]butyl}-5-oxopyrrolidin-1-yl]propyl}thiophene-2-carboxylate (PF-04475270). J Pharmacol Exp Ther. 2009;331(2):627-635. [Content Brief]
- [2]. Prasanna G, et al. Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models. Exp Eye Res. 2009;89(5):608-617. [Content Brief]
Keywords
