1. GPCR/G Protein
  2. Glucocorticoid Receptor
  3. GW-870086

GW-870086 

Cat. No.: HY-103662
Handling Instructions

GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.

For research use only. We do not sell to patients.

GW-870086 Chemical Structure

GW-870086 Chemical Structure

CAS No. : 827319-43-7

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Description

GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.

IC50 & Target

pIC50: 10.1 (glucocorticoid receptor, A549 NF-κB cells)[1]

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)[1]. 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[2].

Clinical Trial
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

Cells are exposed to DEX, PRED, or GW-870086 at 0, 1, 3, 10, 30, 100 or 300 nM for 5 days. Compounds (GW-870086, etc.) are reconstituted in DMSO as 300-mM stock solutions that are diluted to give final drug concentrations in DMEM. Media (DMEM supplemented with 1% FBS) is changed after 48 hours and equal volumes of media from each group are collected after the final 72 hours of treatment, concentrated (×10), and added to an equal volume of ×2 sample buffer. Cells are then rinsed with PBS and scraped directly into 100-μL ×2 sample buffer/well. All samples are incubated at 100°C for 8 minutes and stored at −20°C until analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

559.64

Formula

C₃₁H₃₉F₂NO₆

CAS No.

827319-43-7

SMILES

O=C(C1C(C)(C)C1(C)C)O[[email protected]]2([[email protected]@]3([[email protected]@]([[email protected]@]4([H])[[email protected]@](F)([[email protected]@]5(C([[email protected]@H](F)C4)=CC(C=C5)=O)C)[[email protected]@H](O)C3)([H])C[[email protected]]2C)C)C(OCC#N)=O

Shipping

Room temperature in continental US; may vary elsewhere

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GW-870086
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HY-103662
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Cat. No.: HY-103662