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

Research use only, not for human use.

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

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

In SH-SY5Y cells, GP130 receptor agonist-1 (Compound 2) treatment showed a 2-fold increase in phosphorylation of STAT3 within 10 min at its regulatory Tyr705 site. In primary hippocampal neuronal cultures, the pSTAT3 levels are below levels of detection for GP130 receptor agonist-1 at all time points.GP130 receptor agonist-1 treatment shows 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, andin primary cortical neurons.

For GP130 receptor agonist-1 (Compound 2), 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.

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Others

Other Targets

gp130

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339303-87-6

270.32

C15H11FN2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (369.93 mM)

Fc(cc1)ccc1Nc1nc(-c2ccccc2)cs1

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(-20℃)

With Ice Pack

≥ 2 years