| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GR[2]
GSK9027 targets the glucocorticoid receptor (GR), functioning as a nonsteroidal partial agonist. It binds to the glucocorticoid receptor and modulates its transcriptional activity. On the 2× glucocorticoid response element (GRE) reporter system, GSK9027 behaves as a partial agonist, achieving intrinsic activity relative to the full agonist dexamethasone. The compound inhibits the production of the proinflammatory mediator IL-6 in vivo. Its nonsteroidal nature may offer advantages over traditional steroidal glucocorticoids in terms of side effect profiles. |
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| ln Vitro |
GSK9027 is a partial agonist that exhibits decreased 2×GRE reporter activation[2].
In vitro, GSK9027 demonstrates partial agonist activity on the 2× glucocorticoid response element (GRE) reporter system. It achieves intrinsic activity relative to dexamethasone, indicating that it activates GR-mediated transcription but to a lesser extent than the full agonist. The compound's partial agonist profile may result in a more favorable side effect profile compared to full agonists while maintaining anti-inflammatory efficacy. GSK9027 can be assessed in reporter gene assays using GRE-luciferase constructs and in functional assays measuring the production of pro-inflammatory cytokines such as IL-6. |
| ln Vivo |
In vivo, GSK9027 inhibits the production of the proinflammatory mediator IL-6. The compound has been investigated for the treatment of acute and chronic inflammatory conditions. Its nonsteroidal nature and partial agonist profile may offer advantages over traditional glucocorticoids, potentially reducing the risk of adverse effects such as metabolic disturbances and bone loss. The compound's in vivo efficacy is typically assessed in animal models of inflammation, where endpoints include measurements of inflammatory markers, tissue pathology, and functional outcomes. Further studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for GSK9027 typically involve competitive binding experiments using glucocorticoid receptor and radiolabeled or fluorescently labeled dexamethasone as tracer. The compound's binding affinity to the receptor is assessed, with IC₅₀ or Kd values determined. Its partial agonist activity is confirmed through functional assays measuring GRE-mediated transcriptional activation. The compound's intrinsic activity is expressed relative to dexamethasone. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations and cell-based systems.
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| Cell Assay |
In vitro cell-based assays for GSK9027 utilize cell lines expressing glucocorticoid receptor to assess its partial agonist activity. Cells are treated with varying concentrations of the compound for 24-48 hours. Glucocorticoid receptor-mediated transcriptional activity is evaluated using reporter gene assays with GRE-luciferase constructs. The compound's intrinsic activity is compared to that of dexamethasone. Anti-inflammatory activity is assessed by measuring the production of pro-inflammatory cytokines such as IL-6 in immune cells following stimulation. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
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| Animal Protocol |
In vivo animal studies with GSK9027 typically involve administration of the compound to rodent models of acute or chronic inflammation. Potential study designs include models of inflammatory diseases such as rheumatoid arthritis, asthma, or inflammatory bowel disease. Typical endpoints would include measurements of IL-6 and other inflammatory markers, assessment of tissue pathology, evaluation of immune cell infiltration, and pharmacokinetic profiling. The compound's partial agonist profile may allow for evaluation of its therapeutic index compared to full agonists. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
GSK9027 has a molecular weight of 525.52 g/mol and a molecular formula of C₂₇H₁₉F₄N₃O₂S. Its chemical name is N-{4-[1-(4-fluorophenyl)-1H-indazol-5-yl]-3-(trifluoromethyl)phenyl}-1-phenylmethanesulfonamide. The compound has a calculated LogP of 7.95 and a PSA of 72.37. It is soluble in DMSO at <52.55 mg/mL. As a nonsteroidal glucocorticoid receptor agonist, it may offer advantages in terms of pharmacokinetic properties compared to steroidal glucocorticoids.
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| Toxicity/Toxicokinetics |
GSK9027 is intended for research use only and is not approved for human therapeutic applications. As a research chemical, comprehensive toxicological data are not extensively documented in the publicly accessible literature. Standard safety precautions should be observed when handling this compound, including the use of appropriate personal protective equipment. As with all research chemicals, comprehensive toxicological profiling would be required before any consideration for clinical development. The compound should be handled in well-ventilated areas with proper waste disposal procedures.
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| References |
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| Additional Infomation |
GSK9027 (CAS#: 1229096-88-1) has a molecular formula of C₂₇H₁₉F₄N₃O₂S and a molecular weight of 525.52 g/mol. Its chemical name is N-{4-[1-(4-fluorophenyl)-1H-indazol-5-yl]-3-(trifluoromethyl)phenyl}-1-phenylmethanesulfonamide. It is a nonsteroidal glucocorticoid receptor agonist that behaves as a partial agonist on the 2× GRE reporter system. It achieves intrinsic activity relative to dexamethasone and inhibits IL-6 production in vivo. GSK9027 is used for inflammatory condition research. This compound is not a drug and has not undergone clinical trials.
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| Molecular Formula |
C27H19F4N3O2S
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|---|---|
| Molecular Weight |
525.52
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| Exact Mass |
525.113
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| CAS # |
1229096-88-1
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| PubChem CID |
24882669
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| Appearance |
White to off-white solid powder
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| LogP |
7.946
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
853
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)CS(=O)(=O)NC2=CC(=C(C=C2)C3=CC4=C(C=C3)N(N=C4)C5=CC=C(C=C5)F)C(F)(F)F
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| InChi Key |
DXBJGDVBQPEMOB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H19F4N3O2S/c28-21-7-10-23(11-8-21)34-26-13-6-19(14-20(26)16-32-34)24-12-9-22(15-25(24)27(29,30)31)33-37(35,36)17-18-4-2-1-3-5-18/h1-16,33H,17H2
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| Chemical Name |
N-[4-[1-(4-fluorophenyl)indazol-5-yl]-3-(trifluoromethyl)phenyl]-1-phenylmethanesulfonamide
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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: 250 mg/mL (475.72 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9029 mL | 9.5144 mL | 19.0288 mL | |
| 5 mM | 0.3806 mL | 1.9029 mL | 3.8058 mL | |
| 10 mM | 0.1903 mL | 0.9514 mL | 1.9029 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.
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