| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Glucocorticoid receptor modulator 2 targets the glucocorticoid receptor (GR), functioning as a selective modulator with an IC₅₀ of less than 100 nM. By modulating the glucocorticoid receptor, the compound influences the transcription of glucocorticoid-responsive genes involved in inflammation, immune responses, and various other physiological processes. Selective modulation of the glucocorticoid receptor may offer the potential for anti-inflammatory and immunomodulatory effects with a reduced side effect profile compared to full agonists.
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| ln Vitro |
In vitro, glucocorticoid receptor modulator 2 demonstrates potent modulator activity with an IC₅₀ of less than 100 nM. The compound's activity is assessed in cell-based reporter assays using glucocorticoid response element (GRE)-luciferase constructs to measure receptor-mediated transcriptional modulation. It shows selectivity for the glucocorticoid receptor. The compound can be used to study inflammatory and immune responses in vitro. Its activity is typically compared to that of dexamethasone and other glucocorticoid receptor modulators. Dose-response curves are generated to determine EC₅₀ and IC₅₀ values.
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| ln Vivo |
Specific in vivo activity data for glucocorticoid receptor modulator 2 are not extensively documented in the publicly available literature. As a glucocorticoid receptor modulator with an IC₅₀ of less than 100 nM, the compound has potential applications in the research of inflammatory and immune diseases. It may be investigated in animal models of inflammatory conditions such as rheumatoid arthritis, asthma, or inflammatory bowel disease. However, detailed in vivo pharmacological studies have not been published. Further research is needed to characterize its in vivo efficacy, pharmacokinetics, and safety profile.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for glucocorticoid receptor modulator 2 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 an IC₅₀ of less than 100 nM determined through dose-response binding experiments. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. Binding affinity is expressed as IC₅₀ or Kd values. The compound's modulator activity is confirmed through functional assays measuring GRE-mediated transcriptional modulation.
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| Cell Assay |
In vitro cell-based assays for glucocorticoid receptor modulator 2 utilize cell lines expressing glucocorticoid receptor to assess its modulator 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. Immunomodulatory activity is assessed by measuring the production of pro-inflammatory and anti-inflammatory cytokines in immune cells following stimulation. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed. Dose-response curves are generated to determine EC₅₀ and IC₅₀ values.
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| Animal Protocol |
In vivo animal studies with glucocorticoid receptor modulator 2 would typically involve administration of the compound to rodent models of inflammatory or immune diseases. Potential study designs include models of rheumatoid arthritis, asthma, inflammatory bowel disease, or contact hypersensitivity. Typical endpoints would include measurements of inflammation markers, assessment of tissue pathology, evaluation of immune cell infiltration, and pharmacokinetic profiling. All procedures must comply with institutional animal care and use guidelines. Detailed published in vivo protocols are not currently available.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for glucocorticoid receptor modulator 2 are not extensively documented in the publicly available literature. The compound has a molecular weight of 482.55 g/mol and a molecular formula of C₂₉H₂₇FN₄O₂. Its IUPAC name is N-((2R,3S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)-4.... As a small molecule with reasonable physicochemical properties, it may have suitable characteristics for oral bioavailability, though detailed PK parameters have not been published. Further studies are needed to characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Glucocorticoid receptor modulator 2 is intended for research use only and is not approved for human therapeutic applications. As a research chemical, comprehensive toxicological data are not available 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 | |
| Additional Infomation |
Glucocorticoid receptor modulator 2 (CAS#: 2452396-89-1) has a molecular formula of C₂₉H₂₇FN₄O₂ and a molecular weight of 482.55 g/mol. It is a glucocorticoid receptor modulator with an IC₅₀ of less than 100 nM. The compound is identified as Example 1 in the relevant patent literature. It can be used for research of inflammatory and immune diseases. This compound is not a drug and has not undergone clinical trials for therapeutic use. It is strictly a research reagent for studying glucocorticoid receptor biology and related pathways.
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| Molecular Formula |
C29H27FN4O2
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| Molecular Weight |
482.548690080643
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| Exact Mass |
482.211
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| CAS # |
2452396-89-1
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| PubChem CID |
154598160
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| Appearance |
Light brown to brown solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
833
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| Defined Atom Stereocenter Count |
2
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| SMILES |
FC1C=CC(=CC=1)N1C2C=CC(=CC=2C=N1)N1C(C(C)(C)[C@@H]([C@H]1C1C=CC=CC=1)NC(C1CC1)=O)=O
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| InChi Key |
GJNFFVZYGXQBFZ-CLJLJLNGSA-N
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| InChi Code |
InChI=1S/C29H27FN4O2/c1-29(2)26(32-27(35)19-8-9-19)25(18-6-4-3-5-7-18)33(28(29)36)23-14-15-24-20(16-23)17-31-34(24)22-12-10-21(30)11-13-22/h3-7,10-17,19,25-26H,8-9H2,1-2H3,(H,32,35)/t25-,26-/m1/s1
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| Chemical Name |
N-[(2R,3S)-1-[1-(4-fluorophenyl)indazol-5-yl]-4,4-dimethyl-5-oxo-2-phenylpyrrolidin-3-yl]cyclopropanecarboxamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.0723 mL | 10.3616 mL | 20.7232 mL | |
| 5 mM | 0.4145 mL | 2.0723 mL | 4.1446 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0723 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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