A potent and selective PDE9A inhibitor (IC50s = 65 and 168 nM for the human and rat enzymes

BI-409306 – 5 mg

Brand:
Cayman
CAS:
1189767-28-9
Storage:
-20
UN-No:
Non-Hazardous - /

BI-409306 is a potent and selective phosphodiesterase 9A (PDE9A) inhibitor with IC50 values of 65 and 168 nM for the human and rat enzymes, respectively.{52498} It is selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but does inhibit human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively). BI-409306 (0.5 mg/kg), in combination with MK-801, an NMDA receptor antagonist that reduces cGMP levels, increases cGMP levels by 41% in mouse striatal tissue compared with MK-801 alone. BI 406306 enhances long-term potentiation (LTP) in hippocampal slices and reverses MK-801-induced working memory deficits in a T-maze task in mice when administered at doses ranging from 0.007 to 2.5 mg/kg.  

 

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SKU: 30375 - 5 mg Category:

Description

A potent and selective PDE9A inhibitor (IC50s = 65 and 168 nM for the human and rat enzymes, respectively); selective for PDE9A over PDE2A, -3A, -4B, -5A, -6AB, -7A and -10A and 95 non-PDE targets at 10 µM but inhibits human PDE1A and PDE1C (IC50s = 1.45 and 1.17 µM, respectively); increases mouse striatal cGMP levels at 0.5 mg/kg in combination with MK-801; enhances LTP in hippocampal slices and reverses MK-801-induced working memory deficits in mice at 0.007-2.5 mg/kg

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

Synonyms: 

Molecular weight: 311.3

CAS: 1189767-28-9

Purity: ≥98%

Formulation: A crystalline solid

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