GSK 356278

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

一种有效、选择性、脑渗透性、口服生物可利用的磷酸二酯酶 4 (PDE4) 抑制剂，pIC50 为 8.8 (PDE4B)；同样抑制 PDE4A 和 PDE4D，pIC50 分别为 8.6 和 8.7。

A potent, selective, brain-penetrant and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with pIC50 of 8.8 (PDE4B); equally inhibits PDE4A and PDE4Dwith pIC50 of 8.6 and 8.7, exhibits >100-fold selectivity for PDE4B over the other 10 PDEs; inhibits LPS-induced release of TNF-α in human whole blood with pIC50 of 7.6, demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in models of anxiety.Anxiety Phase 1 Clinical.

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Animal Model:Male Lewis rats (320-400 g) are treated with lipopolysaccharide (LPS)Dosage:0.003-3 mg/kgAdministration:P.o. administration 30 minutes prior to the LPS challengeResult:Reduced the level of neutrophilia in a dose-dependent manner, with an ED50 of 0.09 mg/kg.Animal Model:Male CD rats Dosage:1 mg/kg (Pharmacokinetic Analysis) Administration:I.v. and p.o. administration Result:Oral bioavailability (91%), Cmax (205 nM), T1/2 (2.2 h).

GSK356278 | GSK-356278

Angiogenesis

PDE

PDE

Neurological Disease

Anxiety

720704-34-7

439.538

C21H25N7O2S

>98% (HPLC)

In Vitro:?DMSO : 2.5 mg/mL (5.69 mM)

CCN1N=CC2=C(NC3CCOCC3)C(C4=NN=C(CC5=C(C)N=C(C)S5)O4)=CN=C21

5-(5-((2,4-dimethylthiazol-5-yl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine

(-20℃)

With Ice Pack

≥ 2 years