GP130 receptor agonist-1

产品编号 T9157Cas号 339303-87-6

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

GP130 receptor agonist-1 (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。

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产品编号 T9157别名 N-(4-Fluorophenyl)-4-phenyl-2-thiazolamiCas号 339303-87-6

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生物活性

产品描述	GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.
体外活性	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.
体内活性	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.
别名	N-(4-Fluorophenyl)-4-phenyl-2-thiazolami

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 55 mg/ml (203.46 mM)

溶液配制表

DMSO