Description
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.
Product information
CAS Number: 339303-87-6
Molecular Weight: 270.32
Formula: C15H11FN2S
Chemical Name: N-(4-fluorophenyl)-4-phenyl-1,3-thiazol-2-amine
Smiles: FC1C=CC(=CC=1)NC1=NC(=CS1)C1C=CC=CC=1
InChiKey: RSKMQDIAPGOWDL-UHFFFAOYSA-N
InChi: InChI=1S/C15H11FN2S/c16-12-6-8-13(9-7-12)17-15-18-14(10-19-15)11-4-2-1-3-5-11/h1-10H,(H,17,18)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
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.
Products are for research use only. Not for human use.
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