GW-870086 |
Catalog No.GC31936
One-Click Copy Product Info
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GW-870086 est un agent anti-inflammatoire puissant, agissant comme un agoniste des récepteurs des glucocorticoÏdes, avec un pIC50 de 10,1 dans les cellules A549 exprimant NF-κB.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 827319-43-7
Sample solution is provided at 25 µL, 10mM.
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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.
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].
[1]. Uings IJ, et al. Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile. Br J Pharmacol. 2013 Jul;169(6):1389-403. [2]. Stamer WD, et al. Unique response profile of trabecular meshwork cells to the novel selective glucocorticoid receptor agonist, GW870086X. Invest Ophthalmol Vis Sci. 2013 Mar 1;54(3):2100-7.
Cell experiment: | 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]. |
References: [1]. Uings IJ, et al. Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile. Br J Pharmacol. 2013 Jul;169(6):1389-403. | |
| Cas No. | 827319-43-7 | SDF | |
| Canonical SMILES | O=C(C1C(C)(C)C1(C)C)O[C@]2([C@@]3([C@@]([C@@]4([H])[C@@](F)([C@@]5(C([C@@H](F)C4)=CC(C=C5)=O)C)[C@@H](O)C3)([H])C[C@H]2C)C)C(OCC#N)=O | ||
| Formula | C31H39F2NO6 | M.Wt | 559.64 |
| Solubility | DMSO : 100 mg/mL (178.69 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7869 mL | 8.9343 mL | 17.8686 mL |
| 5 mM | 357.4 μL | 1.7869 mL | 3.5737 mL |
| 10 mM | 178.7 μL | 893.4 μL | 1.7869 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)