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| 5mg |
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| Targets |
Glucocorticoid receptor agonist-3 targets the glucocorticoid receptor (GR), a nuclear receptor that, upon activation by glucocorticoids, translocates to the nucleus and modulates the transcription of anti-inflammatory genes while repressing pro-inflammatory gene expression. The glucocorticoid receptor is a clinically validated target for the treatment of inflammatory and autoimmune diseases, and GR agonists are widely used as anti-inflammatory and immunosuppressive agents.
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| ln Vitro |
As a glucocorticoid receptor agonist, Glucocorticoid receptor agonist-3 shows in vitro activity by activating the glucocorticoid receptor and modulating gene expression. The compound is expected to exert anti-inflammatory effects through transactivation of anti-inflammatory genes and transrepression of pro-inflammatory genes. The specific EC50 for glucocorticoid receptor activation has not been detailed in the available literature.
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| ln Vivo |
In vivo activity of Glucocorticoid receptor agonist-3 has been suggested based on its mechanism of action as a glucocorticoid receptor agonist. Glucocorticoid receptor agonists are widely used in vivo for the treatment of inflammatory and autoimmune diseases. However, detailed in vivo efficacy data for this specific compound have not been extensively reported in the available literature.
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| Enzyme Assay |
Non-cell-based binding assays for Glucocorticoid receptor agonist-3 typically involve measuring the affinity of the compound for the glucocorticoid receptor using radioligand binding or fluorescence polarization assays. A standard protocol includes: incubating purified glucocorticoid receptor protein with a radiolabeled or fluorescently labeled glucocorticoid ligand, adding Glucocorticoid receptor agonist-3 at various concentrations, and measuring displacement of the labeled ligand to determine binding affinity (Ki or Kd).
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| Cell Assay |
Cell-based assays for Glucocorticoid receptor agonist-3 typically involve cell lines expressing the glucocorticoid receptor, such as A549 lung epithelial cells or primary immune cells. A representative protocol includes: culturing cells in appropriate medium, treating with Glucocorticoid receptor agonist-3 at various concentrations (0.001–100 μM) for 24–72 hours, and measuring glucocorticoid receptor activation using reporter gene assays (e.g., GRE-luciferase). Anti-inflammatory activity can be assessed by measuring cytokine production (e.g., IL-6, TNFα) by ELISA following inflammatory stimulation.
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| Animal Protocol |
In vivo animal studies with Glucocorticoid receptor agonist-3 would typically involve mouse models of inflammatory or autoimmune diseases, such as carrageenan-induced paw edema, collagen-induced arthritis, or LPS-induced endotoxemia. A typical protocol involves administering the compound via oral gavage or intraperitoneal injection at doses determined from pharmacokinetic studies, followed by assessment of inflammatory markers, histopathological analysis of target tissues, and evaluation of clinical disease scores.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Glucocorticoid receptor agonist-3 have not been extensively reported in the available literature. The compound has a molecular weight of 617.70 g/mol and a molecular formula of C36H40FNO7. Storage: Powder at -20°C for 3 years, in solvent at -80°C for 1 year. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
As a research compound, Glucocorticoid receptor agonist-3 is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity.
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| References | |
| Additional Infomation |
Glucocorticoid receptor agonist-3 (Preparation 6, CAS 2842165-73-3) is a glucocorticoid receptor agonist. It has a molecular formula of C36H40FNO7 and a molecular weight of 617.70 g/mol. The compound is available for research applications in the study of glucocorticoid receptor signaling and inflammatory diseases.
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| Exact Mass |
617.279
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| CAS # |
2842165-73-3
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| PubChem CID |
165384889
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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-ZGWDLKLYSA-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,6S,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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