GSK 356278

Research use only, not for human use.

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.

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.

——

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