2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. 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.

For research use only. We do not sell to patients.

PF-04475270

PF-04475270 Chemical Structure

CAS No. : 1201925-19-0

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PF-04475270 Related Antibodies

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Description

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].

IC50 & Target[1]

hEP4

2 nM (IC50)

dog EP4

8 nM (IC50)

In Vitro

PF-04475270 crosses cornea tissue more robustly than its active metabolite CP-734432[1].
PF-04475270 (10 μM) is rapidly converted to CP-734432 in rabbit corneal homogenates[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-04475270 Related Antibodies
In Vivo

PF-04475270 (0.1-5 μg; topical administration; single instillation; 0.5-1.25 μg; topical administration; once daily; for 4 consecutive days) reduces intraocular pressure (IOP) in normotensive beagle dogs, with a better IOP-lowering effect observed after single administration[1][2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Beagle dogs (male and female)[1][2]
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)
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)
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.
Molecular Weight

511.60

Formula

C26H32F3NO4S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-04475270 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-044752701201925-19-0PF04475270PF 04475270Prostaglandin ReceptorEP4 prostaglandin receptorcAMPβ-lactamaseocular esterasesBeagle dogshuman corneal epithelial modelscAMP response elementcorneal homogenatesrabbit corneasglaucomaInhibitorinhibitorinhibit

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