| Identification | Back Directory | [Name]
TAK-915 | [CAS]
1476727-50-0 | [Synonyms]
TAK-915
(S)-N-(1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
Pyrido[2,3-b]pyrazine-4(1H)-carboxamide, N-[(1S)-1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-methoxyethyl]-2,3-dihydro-7-methoxy-2-oxo- | [Molecular Formula]
C19H18F4N4O5 | [MDL Number]
MFCD32219404 | [MOL File]
1476727-50-0.mol | [Molecular Weight]
458.36 |
| Chemical Properties | Back Directory | [Boiling point ]
651.0±55.0 °C(Predicted) | [density ]
1.420±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
11.20±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment[1][2]. | [in vivo]
TAK-915 (3 mg/kg; oral administration; daily; for 4 days; male F344 rats) treatment significantly reduces escape latency in aged rats in the Morris water maze task[2].
TAK-915 (1, 3, and 10 mg/kg, p.o.) dose-dependently attenuates the non-selective muscarinic antagonist scopolamine-induced memory deficits in rats[2].
Oral dosing of TAK-915 (compound 36) (3 or 10 mg/kg) in mice produces a dose-dependent increase in 3',5'-cyclic guanosine monophosphate (cGMP) levels, with significant cGMP increases observed at a dose of 10 mg/kg[1]. | Animal Model: | Male F344 rats (10-week-old and 26-month-old) bearing morris water maze task[2] | | Dosage: | 3 mg/kg | | Administration: | Oral administration; daily; for 4 days | | Result: | Significantly reduced escape latency in aged rats in the Morris water maze task.
|
| [IC 50]
PDE2A: 0.61 nM (IC50); PDE1A: 2497 nM (IC50) | [References]
[1] Mikami S, et al. Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders. J Med Chem. 2017 Sep 28;60(18):7677-7702. DOI:10.1021/acs.jmedchem.7b00807
[2] Nakashima M, et al. TAK-915, a phosphodiesterase 2A inhibitor, ameliorates the cognitive impairment associated with aging in rodent models. Behav Brain Res. 2019 Dec 30;376:112192. DOI:10.1016/j.bbr.2019.112192 |
|
| Company Name: |
ChemShuttle, Inc.
|
| Tel: |
0150-83588313-811 18800520310 |
| Website: |
www.jiehuapharma.com/ |
|