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

Item Number

P288577

Grouped product items
SKU	Size	Availability	Price	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

Potent and selective PDE2A inhibitor

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Basic Description

Synonyms	AKOS028114948 \| 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 & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent and selective PDE2A inhibitor (IC50= 1 nM). Exhibits 2000-fold selectivity for PDE2A over PDE10A. Brain penetrant.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of phosphodiesterase 2A

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

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]

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Basic Description