A PDE9A inhibitor (IC50 = 22 nM); is selective for PDE9A over PDE1C (IC50 = >1

PF-04449613 – 5 mg

Brand:
Cayman
CAS:
1236858-52-8
Storage:
-20
UN-No:
Non-Hazardous - /

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.  

 

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SKU: 30946 - 5 mg Category:

Description

A PDE9A inhibitor (IC50 = 22 nM); is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM); increases cGMP CSF levels in rats; increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo at 10 mg/kg; increases the average running speed of mice in an accelerating rotarod task at 10 mg/kg

Formal name: 1,5-dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one

Synonyms: 

Molecular weight: 395.5

CAS: 1236858-52-8

Purity: ≥98%

Formulation: A solid

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