PF 05180999

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Cat.No. 6405 - PF 05180999 | C19H17F3N8 | CAS No. 1394033-54-5
Description: Potent and selective PDE2A inhibitor
Chemical Name: 4-(1-Azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-imidazo[5,1-f][1,2,4]triazine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective PDE2A inhibitor (IC50 = 1 nM). Exhibits 2000-fold selectivity for PDE2A over PDE10A. Brain penetrant.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 414.39
Formula C19H17F3N8
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1394033-54-5
PubChem ID 60143346
InChI Key CLGCHUKGBICQTE-UHFFFAOYSA-N
Smiles CC1=NC(C2=C(C3=NC=C(C(F)(F)F)C=C3)N(C)N=C2)=C4N1N=CN=C4N5CCC5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.72 50
ethanol 20.72 50

Preparing Stock Solutions

The following data is based on the product molecular weight 414.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.41 mL 12.07 mL 24.13 mL
5 mM 0.48 mL 2.41 mL 4.83 mL
10 mM 0.24 mL 1.21 mL 2.41 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Mikami et al (2017) Discovery of orally bioavailable brain penetrating in vivo active phosphodiesterase 2a inhibitor series for the treatment of cognitive disorders. J.Med.Chem. 60 7658 PMID:


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