GW-870086

SKU: orb1219520

Description

GW-870086 is an effective anti-inflammatory agent. GW-870086 also plays a role in a glucocorticoid receptor agonist (pIC50: 10.1 in A549 cells expressing NF-κB). GW-870086 (10-100 nM) obviously increases fibronectin secretion. GW-870086 (1 pM-1 μM) dose-dependently inhibits the L-6 release induced by TNF-α in A549 epithelial carcinoma cells and by IL-1 in MG63 osteosarcoma cells (pIC50s, 9.6, 10.2). GW-870086 displays no effect on the MMTV reporter genes in A549 cells and has little or no activity at the oestrogen receptor, progesterone receptor, progesterone receptor, mineralocorticoid receptor, or androgen receptor. GW-870086 also has no effect on MMP2 secretion and does not enhance cellular myocilin.

Key Properties

• CAS Number: 827319-43-7
• MW: 559.64
• Purity: >98% (HPLC)
• Formula: C₃₁H₃₉F₂NO₆
• SMILES: [H][C@@]12C[C@@H](C)[C@](OC(=O)C3C(C)(C)C3(C)C)(C(=O)OCC#N)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])C[C@H](F)C2=CC(=O)C=C[C@]12C
• Target: glucocorticoid receptor
• Solubility: In Vitro: DMSO : 100 mg/mL (178.69 mM)

Bioactivity

• In Vitro:
  GW-870086 a glucocorticoid receptor agonist, inhibits NFkB reporter gene with a pIC50 of 10.1, but shows no effect on the MMTV reporter genes in A549 cells, and has little or no activity at the oestrogen receptor, progesterone receptor, progesterone receptor, mineralocorticoid receptor or androgen receptor. GW-870086 (1 pM-1 μM) dose-dependently inhibits the L-6 release induced by TNF-α in A549 epithelial carcinoma cells and by IL-1 in MG63 osteosarcoma cells (pIC50s, 9.6, 10.2). GW-870086 (GW870086X; 10-100 nM) significantly increases fibronectin secretion. However, GW-870086 has no effect on MMP2 secretion, and does not increase cellular myocilin.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

glucocorticoid receptor