GP130 receptor agonist-1 是一种有效的、可透过血脑屏障并具有口服活性的 GP130 受体激动剂。GP130 receptor agonist-1 对 NMDA 诱导的神经毒性具有神经保护作用。

GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity.

Solid

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, and in primary cortical neurons. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Mohammad Parvez Alam,et al. A Small Molecule Mimetic of the Humanin Peptide as a Candidate for Modulating NMDA-Induced Neurotoxicity. ACS Chem Neurosci. 2018 Mar 21;9(3):462-468.

In Vitro: DMSO : 100 mg/mL (369.93 mM; Need ultrasonic)配制储备液