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| 25mg |
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Purity: ≥98%
GW-870086 is a novel and potent glucocorticoid receptor agonist that has anti-inflammatory properties, and thus can be potentially usef for the treatment of asthma and atopic dermatitis.. It acts as a glucocorticoid receptor agonist with a pIC50 of 10.1 in A549 cells expressing NF-κB.
| ln Vitro |
The glucocorticoid receptor agonist GW-870086 has a pIC50 of 10.1 and suppresses the NFkB reporter gene; however, it has no effect on the MMTV reporter gene in A549 cells, nor on the progesterone or estrogen receptors. little or nonexistent action at androgen or mineralocorticoid receptors. GW-870086 (1 pM-1 μM) suppresses IL-1-induced L-6 release in MG63 osteosarcoma cells and dose-dependently TNF-α in A549 epithelial cancer cells (pIC50s, 9.6, 10.2)[1]. GW-870086 (GW870086X; 10-100 nM) dramatically boosts the release of fibronectin. GW-870086, however, does not enhance cellular myofibrillar protein or affect MMP2 secretion [2].
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| References |
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| Additional Infomation |
GW870086X has been investigated for the treatment of ASTHMA.
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| Molecular Formula |
C31H39F2NO6
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|---|---|
| Molecular Weight |
559.641276597977
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| Exact Mass |
559.275
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| Elemental Analysis |
C, 66.53; H, 7.02; F, 6.79; N, 2.50; O, 17.15
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| CAS # |
827319-43-7
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| PubChem CID |
11376392
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| Appearance |
White to off-white solid powder
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| LogP |
4.582
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
1280
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| Defined Atom Stereocenter Count |
9
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| SMILES |
O([C@@]1([C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(C=C[C@]4(C)[C@]3([C@H](C[C@]12C)O)F)=O)C(=O)OCC#N)C(C1C(C)(C)C1(C)C)=O
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| InChi Key |
WUBKGTSFJSEIEM-NSHBDUGJSA-N
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| InChi Code |
InChI=1S/C31H39F2NO6/c1-16-12-18-19-14-21(32)20-13-17(35)8-9-28(20,6)30(19,33)22(36)15-29(18,7)31(16,25(38)39-11-10-34)40-24(37)23-26(2,3)27(23,4)5/h8-9,13,16,18-19,21-23,36H,11-12,14-15H2,1-7H3/t16-,18+,19+,21+,22+,28+,29+,30+,31+/m1/s1
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| Chemical Name |
Androsta-1,4-diene-17-carboxylic acid, 6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(((2,2,3,3-tetramethylcyclopropyl)carbonyl)oxy)-, cyanomethyl ester, (6alpha,11beta,16alpha,17alpha)-
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| Synonyms |
GW-870086; GW-870086X; 870086; GW870086; GW870086X; GW 870086; GW 870086X
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~178.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7869 mL | 8.9343 mL | 17.8686 mL | |
| 5 mM | 0.3574 mL | 1.7869 mL | 3.5737 mL | |
| 10 mM | 0.1787 mL | 0.8934 mL | 1.7869 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 GW870086 shows a range of activity on glucocorticoid-up-regulated genes compared with classical glucocorticoids in A549 cells.Br J Pharmacol.2013 Jul;169(6):1389-403. |
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 Effects of GW870086 on respiratory epithelial cell function.Br J Pharmacol.2013 Jul;169(6):1389-403. |
 GW870086 antagonizes the effect of dexamethasone on the MMTV reporter gene.
GW870086 retains transrepressive activity in A549 cells compared with classical glucocorticoids.Br J Pharmacol.2013 Jul;169(6):1389-403. |
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