| Description | GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist. |
| In vitro | 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. |
| In vivo | 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. |
| Synonyms | N-(4-Fluorophenyl)-4-phenyl-2-thiazolami |
| molecular weight | 270.32 |
| Molecular formula | C15H11FN2S |
| CAS | 339303-87-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/ml (203.46 mM) |
| References | 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. |
| Citations | 1. Zhou S, Li Z, Li X, et al.Crosstalk between endothelial cells and dermal papilla entails hair regeneration and angiogenesis during aging.Journal of Advanced Research.2024 |