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PF 05180999 - ≥98%(HPLC), high purity , CAS No.1394033-54-5, Inhibitor of phosphodiesterase 2A

  • Moligand™
  • ≥98%(HPLC)
Item Number
P288577
Grouped product items
SKUSizeAvailabilityPrice Qty
P288577-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$78.90
P288577-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$286.90
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Potent and selective PDE2A inhibitor

View related series
phosphodiesterase 2A Inhibitor

Basic Description

Synonyms1394033-54-5|PF-05180999|PF 05180999|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|PF-999|5L84K4IEN9|4-(1-Azetidinyl)-7-methyl-5-(1-methyl-5-(5-(trifluoromethyl)-2-pyridinyl)-1H-py
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent and selective PDE2A inhibitor (IC50= 1 nM). Exhibits 2000-fold selectivity for PDE2A over PDE10A. Brain penetrant.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of phosphodiesterase 2A

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2B6 Tchem Cytochrome P450 2B6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE2A Tclin cGMP-dependent 3',5'-cyclic phosphodiesterase 6 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AOX1 Tchem Aldehyde oxidase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-(azetidin-1-yl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]pyrazol-4-yl]imidazo[5,1-f][1,2,4]triazine
INCHI InChI=1S/C19H17F3N8/c1-11-27-15(17-18(29-6-3-7-29)24-10-26-30(11)17)13-9-25-28(2)16(13)14-5-4-12(8-23-14)19(20,21)22/h4-5,8-10H,3,6-7H2,1-2H3
InChi Key CLGCHUKGBICQTE-UHFFFAOYSA-N
Canonical SMILES CC1=NC(=C2N1N=CN=C2N3CCC3)C4=C(N(N=C4)C)C5=NC=C(C=C5)C(F)(F)F
Isomeric SMILES CC1=NC(=C2N1N=CN=C2N3CCC3)C4=C(N(N=C4)C)C5=NC=C(C=C5)C(F)(F)F
PubChem CID 60143346
Molecular Weight 414.39

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 20.72, Max Conc. mM: 50; Solvent:ethanol, Max Conc. mg/mL: 20.72, Max Conc. mM: 50

Safety and Hazards(GHS)

RIDADR UN28116.1/PGIII

Related Documents

 SDS

 Specification Sheet

References

1. Mikami S, Sasaki S, Asano Y, Ujikawa O, Fukumoto S, Nakashima K, Oki H, Kamiguchi N, Imada H, Iwashita H et al..  (2017)  Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders..  J Med Chem,  60  (18): (7658-7676).  [PMID:28759228]
2. Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM et al..  (2018)  Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate..  J Med Chem,  61  (3): (1001-1018).  [PMID:29293004]

Solution Calculators

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