N-(4-Fluorophenyl)-4-phenyl-2-thiazolami 是一种有效的、口服有活性的、可透过血脑屏障的GP130受体激动剂。它对 NMDA 诱导的神经毒性具有神经保护作用。

N-(4-Fluorophenyl)-4-phenyl-2-thiazolami is a potent, brain-penetrant and orally active GP130 receptor agonist.

Compound 2 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) treatment showed a 2-fold increase in phosphorylation of STAT3 within 10 min at its regulatory Tyr705 site in SH-SY5Y cells.. Compound 2 treatment increases phosphorylation of AKT at its regulatory Thr308 site and phosphorylation of ERK1/2 at its regulatory Thr202/Tyr204 site in the serum free media condition in SH-SY5Y cells, and in primary cortical neurons.

For Compound 2 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami), mice are dosed orally at 10 or 30 mg/kg, or injected subcutaneously (SQ) at 10 mg/kg, and euthanized after 1, 2, 4, 6, and 8 h post dose. At 2 h after SQ delivery at 10 mg/kg the brain Cmax is 161 ng/g while dosing at 30 mg/kg orally, results in the brain Cmax of 156 ng/g (0.57 μM). The brain to plasma ratio for 2 is ～4:1 for oral 30 mg/kg and ～7.5:1 for 10 mg/kg SQ injection.

339303-87-6

C15H11FN2S

270.33

N-(4-Fluorophenyl)-4-phenyl-2-thiazolami

DMSO:55 mg/ml (203.46 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years