| Name | GP130 receptor agonist-1 |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 55 mg/mL (203.46 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2.5 mg/mL (9.25 mM), Sonication is recommended.
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| Keywords | penetrant | NMDA | neuroprotective | Interleukin Related | Interleukin | Inhibitor | inhibit | GP130 receptor agonist-1 | GP-130 receptor agonist-1 | GP130 receptor agonist1 | GP130 receptor agonist 1 | gp130 | brain |
| Inhibitors Related | Kaolin | Undecane | Fluorene | Ethyl palmitate | Rhamnose monohydrate | Isostearic acid | D(+)-Raffinose pentahydrate | Hydroxypropyl Cellulose | 1,8-Cineole | Tributyrin | Gluconate Calcium | Magnesium sulfate |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | CNS-Penetrant Compound Library | Neuroprotective Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
