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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- CAS No.: 1201925-19-0
- Formule: C26H32F3NO4S
- Masse moléculaire:511.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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hEP4 2 nM (IC50) |
dog EP4 8 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:0.1 μg; 0.25 μg; 2.5 μg; 5 μg (single dose); 0.5 μg; 1.25 μg (once daily for 4 days)
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Administration:topical; single instillation (for 0.1 μg, 0.25 μg, 2.5 μg, 5 μg); once daily; 4 days (for 0.5 μg, 1.25 μg)
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Result:Achieved mean IOP of 73% of baseline at 24 hours post-first dose, 67% of baseline at 48 hours, 65% of baseline at 72 hours, and 65% of baseline at 96 hours for the 0.5 μg multiple-dose group.
Achieved mean IOP of 81% of baseline at 24 hours post-first dose, 64% of baseline at 48 hours, 61% of baseline at 72 hours, and 58% of baseline at 96 hours for the 1.25 μg multiple-dose group.
Demonstrated progressively greater IOP reduction with repeated daily dosing despite no accumulation of the active metabolite CP-734432 in ocular tissues.
Showed a population-based pharmacokinetic-pharmacodynamic model (model II) with a positive feedback loop captured time-dependent IOP lowering, with key parameters including a SC50 of 0.674 ng/g, a Sₘₐₓ of 0.287, and a kₘₒd of 0.029 h-1.
Chemical Information
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CAS No. 1201925-19-0
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Masse moléculaire 511.60
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Formule C26H32F3NO4S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-04475270 Related Classifications
HY-185643 Related Classifications
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