| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Glucocorticoid receptor (GR). The glucocorticoid receptor is a nuclear receptor that binds glucocorticoid hormones and regulates gene expression. Upon ligand binding, GR translocates to the nucleus and modulates transcription of target genes involved in inflammation, metabolism, and cell survival. Glucocorticoid receptor agonists are widely used as anti-inflammatory and immunosuppressive agents.
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| ln Vitro |
Glucocorticoid receptor agonist-4 is a selective agonist for the glucocorticoid receptor. It activates GR signaling, leading to anti-inflammatory effects by suppressing pro-inflammatory cytokine production and promoting anti-inflammatory gene expression. It can be conjugated to TNF-α antibodies for targeted delivery to sites of inflammation. Detailed in vitro activity data (EC50, IC50) are not provided.
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| ln Vivo |
Glucocorticoid receptor agonist-4 has potential applications in autoimmune and inflammatory diseases. By targeting glucocorticoid receptor signaling, it can suppress inflammation and immune responses. Conjugation to TNF-α antibodies enables targeted delivery to inflamed tissues, potentially improving efficacy and reducing systemic side effects. In vivo efficacy would depend on the specific antibody conjugate and disease model.
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| Enzyme Assay |
In vitro receptor binding assays are performed using radiolabeled glucocorticoid (e.g., 3H-dexamethasone) incubated with glucocorticoid receptor protein or cell lysates in the presence of varying concentrations of Glucocorticoid receptor agonist-4. Bound radioactivity is measured by scintillation counting, and IC50 or Ki values are determined from competition binding curves.
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| Cell Assay |
Cell-based reporter assays are performed using cells transfected with glucocorticoid receptor-responsive luciferase reporter constructs and treated with Glucocorticoid receptor agonist-4 at varying concentrations. Luciferase activity is measured to determine EC50 for GR activation. Anti-inflammatory activity is assessed by measuring cytokine production (e.g., TNF-α, IL-6, IL-1β) in immune cells stimulated with LPS.
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| Animal Protocol |
Animal models of autoimmune or inflammatory diseases (e.g., collagen-induced arthritis, experimental autoimmune encephalomyelitis, or inflammatory bowel disease) are administered Glucocorticoid receptor agonist-4 or its antibody conjugates. Disease severity, inflammation markers, and tissue histopathology are assessed to evaluate efficacy. Conjugation to TNF-α antibodies may enhance targeting to inflamed tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Glucocorticoid receptor agonist-4 depend on whether it is administered as a free compound or conjugated to an antibody. As a small molecule, it is expected to have reasonable oral bioavailability and tissue distribution. Antibody conjugation would significantly alter PK, with longer half-life and targeted tissue distribution. Detailed PK data are not available in the literature.
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| Toxicity/Toxicokinetics |
Toxicological data for Glucocorticoid receptor agonist-4 are not available. As a glucocorticoid receptor agonist, it may have side effects similar to other glucocorticoids, including immunosuppression, hyperglycemia, osteoporosis, and adrenal suppression. Targeted delivery via antibody conjugation may reduce systemic toxicity. Standard toxicology studies are required for therapeutic development.
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| References | |
| Additional Infomation |
Glucocorticoid receptor agonist-4 is a research-grade compound for studying glucocorticoid receptor signaling and inflammation. CAS: 2842165-72-2. Molecular formula: C36H40FNO7, molecular weight: 617.70. Synonyms: Compound Preparation 5. It can be conjugated to TNF-α antibodies for autoimmune and inflammatory disease research. For research use only, not for human therapeutic use.
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| Exact Mass |
617.279
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|---|---|
| CAS # |
2842165-72-2
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| PubChem CID |
165145275
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
45
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| Complexity |
1260
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC1=C(C(=C(C=C1)OCC2=CC(=CC=C2)N)F)[C@@H]3O[C@@H]4C[C@H]5[C@@H]6CCC7=CC(=O)C=C[C@@]7([C@H]6[C@H](C[C@@]5([C@@]4(O3)C(=O)CO)C)O)C
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| InChi Key |
HNGDCWMBBDBZCI-ALOVAHRDSA-N
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| InChi Code |
InChI=1S/C36H40FNO7/c1-19-7-10-27(43-18-20-5-4-6-22(38)13-20)32(37)30(19)33-44-29-15-25-24-9-8-21-14-23(40)11-12-34(21,2)31(24)26(41)16-35(25,3)36(29,45-33)28(42)17-39/h4-7,10-14,24-26,29,31,33,39,41H,8-9,15-18,38H2,1-3H3/t24-,25-,26-,29+,31+,33+,34-,35-,36+/m0/s1
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| Chemical Name |
(1S,2S,4R,6R,8S,9S,11S,12S,13R)-6-[3-[(3-aminophenyl)methoxy]-2-fluoro-6-methylphenyl]-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~200 mg/mL (~323.78 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 50.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
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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