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GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $41 | In Stock | In Stock | |
| 10 mg | $65 | In Stock | In Stock | |
| 25 mg | $128 | In Stock | In Stock | |
| 50 mg | $238 | In Stock | In Stock | |
| 100 mg | $345 | In Stock | In Stock | |
| 200 mg | $470 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $58 | In Stock | In Stock |
| 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 |
| Formula | C15H11FN2S |
| Cas No. | 339303-87-6 |
| Smiles | FC1=CC=C(NC2=NC(=CS2)C2=CC=CC=C2)C=C1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (203.46 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 2.5 mg/mL (9.25 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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