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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 | Availability | Quantity |
---|---|---|---|
5 mg | $41 | In Stock | |
10 mg | $65 | In Stock | |
25 mg | $128 | In Stock | |
50 mg | $238 | In Stock | |
100 mg | $345 | In Stock | |
200 mg | $470 | In Stock | |
1 mL x 10 mM (in DMSO) | $58 | 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. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/ml (203.46 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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