2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PF-04822163

PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC50 values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease.

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

PF-04822163 Chemical Structure

PF-04822163 Chemical Structure

CAS No. : 1798334-07-2

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PF-04822163 Related Antibodies

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Description

PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC50 values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease[1].

IC50 & Target

PDE1A

2 nM (IC50)

PDE1B

2.4 nM (IC50)

PDE1C

7 nM (IC50)

PDE2A

5895 nM (IC50)

PDE3A

>30000 nM (IC50)

PDE4D3

7620 nM (IC50)

PDE5A1

>30000 nM (IC50)

PDE7B

>29800 nM (IC50)

PDE9A1

>30000 nM (IC50)

PDE10A1

252 nM (IC50)

PDE11A4

8257 nM (IC50)

In Vivo

PF-04822163 (10 mg/kg; p.o.; single dose) achieved a Tmax of 274 ng/mL in rat plasma at 0.5 h, with a terminal half-life of 5.5 h, and showed blood-brain barrier permeability[1].

Pharmacokinetic parameters in rat[1]

species route dose Tmax(h) t1/2(h) fu B/P CSF/Pu
rat p.o. 10 mg/kg 0.5 - 0.028 3.4 1.7

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

340.80

Formula

C19H17ClN2O2
CAS No.
SMILES

COC1=C(OC)C=CC2=C([C@H]3CCC4=C3C=C(Cl)C=C4)N=CN=C12
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-04822163 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-048221631798334-07-2PF04822163PF 04822163Phosphodiesterase (PDE)blood-brain barrierattention deficit hyperactivity disorderParkinson's diseaseInhibitorinhibitorinhibit

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