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

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

SynonymsAKOS028114948 | BP166579 | SCHEMBL11971205 | 1394033-54-5 | 5L84K4IEN9 | compound 30 [PMID: 29293004] | CS-0039866 | UNII-5L84K4IEN9 | 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
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(Human)

PDE2A Tclin cGMP-dependent 3',5'-cyclic phosphodiesterase (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AOX1 Tchem Aldehyde oxidase (429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver (3974 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A (122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

PDE2A Phosphodiesterase 2A (77 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Brain (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDCKII-LE (120 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

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] [10.1021/op500134e]
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] [10.1021/op500134e]

Solution Calculators

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