TAK-915

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TAK-915 (TAK915) 是一种高效、选择性、脑穿透性、口服活性的磷酸二酯酶 2A (PDE2A) 抑制剂，IC50 为 0.61 nM。

TAK-915 (TAK915) is a highly potent, selective, brain-penetrating and orally active phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 0.61 nM; dispalys 4100-fold selectivity over PDE1A, and >20,000-fold over other PDE isoforms; robustly increased cGMP levels in the rat brain, attenuates MK-801-induced episodic memory deficits in rats. Schizophrenia Phase 1 Clinical.

——

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.TAK-915 (1, 3, and 10?mg/kg, p.o.) dose-dependently attenuates the non-selective muscarinic antagonist scopolamine-induced memory deficits in rats. 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. Animal Model:Male F344 rats (10-week-old and 26-month-old) bearing morris water maze task 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.

TAK915 | TAK 915

Angiogenesis

PDE

PDE

Neurological Disease

Schizophrenia

1476727-50-0

458.37

C19H18F4N4O5

>98% (HPLC)

In Vitro:?DMSO : 7.5 mg/mL (16.36 mM)

O=C(N1C2=NC=C(OC)C=C2NC(C1)=O)N[C@@H](C3=CC=C(OC(F)(F)F)C(F)=C3)COC

N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide

(-20℃)

With Ice Pack

≥ 2 years