GP130 receptor agonist-1

SKU: orb1298321

Description

GP130 receptor agonist-1 is a potent, orally bioavailable, and brain-penetrant small molecule activator of the GP130 receptor. It is a valuable research tool for studying IL-6 cytokine family signaling in both cellular assays and animal models of neuroinflammation and neuroprotection.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 339303-87-6
• MW: 270.32
• Purity: 99.70% (May vary between batches)
• Formula: C₁₅H₁₁FN₂S
• SMILES: FC1=CC=C(NC2=NC(=CS2)C2=CC=CC=C2)C=C1
• Target: Interleukin
• Solubility: DMSO:55 mg/mL (203.46 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (9.25 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

brain, N-(4-Fluorophenyl)-4-phenyl-2-thiazolami, neuroprotective, NMDA, Inhibitor, inhibit, GP130, GP130 receptor agonist 1, GP130 receptor agonist1, GP-130 receptor agonist-1, GP130 receptor agonist-1, gp130, Interleukin Related, Interleukin, penetrant

Compound Identifiers

PubChem CID

623055