AMG-579( AMG 579 | AMG579 )

Catalog No. M10873 CAS No. 1227067-61-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

AMG-579
Note

Research use only, not for human use.
Brief Description

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM.
Description

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM; displays high selectivity with IC50 > 30 uM against all other PDE isoforms; demonstrates excellent target occupancy efficacy in PCP-LMA behavioral model.Schizophrenia Phase 1 Clinical.
In Vitro

——
In Vivo

AMG 579 shows statistically significant reduction of PCP induced behavior in rats over the 2 h period. Minimum effective doses for efficacy in PCP-LMA model is determined to be 0.3 mg/kg for AMG 579. In dog, 5 exhibits superior oral bioavailability of 72%.
Synonyms

AMG 579 | AMG579
Pathway

Angiogenesis
Target

PDE
Recptor

PDE
Research Area

Neurological Disease
Indication

Schizophrenia

CAS Number

1227067-61-9
Formula Weight

441.491
Molecular Formula

C25H23N5O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 41.67 mg/mL (94.39 mM)
SMILES

O=C(C1=CC=C(OC2=NC=CN=C2C3CCN(C(C)=O)CC3)C=C1)C4=NC5=CC=CC=C5N4
Chemical Name

1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone

1. Hu E, et al. J Med Chem. 2014 Aug 14;57(15):6632-41.

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