Glucocorticoid receptor modulator 1
Based on 1 Customer Validation
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.
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- Pureza : 99.67%
- No. CAS: 2868357-11-1
- Fòrmula: C24H23ClN2O4S
- Peso molecular:470.97
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 9 nM (NF-κB), 130 nM (AP-1)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Peritoneal macrophage | IC50 |
6.9 μM
Compound: B-53
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Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA
Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA
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[PMID: 36399795] |
| Peritoneal macrophage | IC50 |
7.74 μM
Compound: B-53
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Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA
Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA
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[PMID: 36399795] |
In Vitro
Glucocorticoid receptor modulator 1 (compound B53) shows inhibitory activities against NF-κB and AP-1 with IC50s of 9 nM and 130 nM, respectively[1].
Glucocorticoid receptor modulator 1 (10 μM; 24 h) decreases the mRNA expression of the inflammatory factors of IL-6, IL-1β, TSLP, MMP-13, TNF-α, and CCL-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse macrophage RAW264.7 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Practically decreased the mRNA expression of the inflammatory factors of IL-6, IL-1β, TSLP, MMP-13, TNF-α, and CCL-2.
Reduced IL-6 and TNF-α dose-dependently with IC50s of 6.90 μM and 7.74 μM, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/C mice (5 weeks; 2,4-dinitrochlorobenzene-induced atopic dermatitis model)[1]
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Dosage:5, 10 and 20 mg/kg
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Administration:p.o.; for 24 days
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Result:Significantly improved the skin damage in a dose-dependent manner, and suppressed inflammatory factors of IL-6, IL-1β, TSLP, and MMP-13.
Chemical Information
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No. CAS 2868357-11-1
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Appearance Solid
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Peso molecular 470.97
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Fòrmula C24H23ClN2O4S
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Color White to off-white
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SMILES
COC1=C(C=C(C(C)=C1)Cl)S(=O)(NC2=CC=C3C(CCCN3C(C4=CC=CC=C4)=O)=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (212.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1233 mL | 10.6164 mL | 21.2328 mL | 53.0819 mL |
| 5 mM | 0.4247 mL | 2.1233 mL | 4.2466 mL | 10.6164 mL | |
| 10 mM | 0.2123 mL | 1.0616 mL | 2.1233 mL | 5.3082 mL | |
| 15 mM | 0.1416 mL | 0.7078 mL | 1.4155 mL | 3.5388 mL | |
| 20 mM | 0.1062 mL | 0.5308 mL | 1.0616 mL | 2.6541 mL | |
| 25 mM | 0.0849 mL | 0.4247 mL | 0.8493 mL | 2.1233 mL | |
| 30 mM | 0.0708 mL | 0.3539 mL | 0.7078 mL | 1.7694 mL | |
| 40 mM | 0.0531 mL | 0.2654 mL | 0.5308 mL | 1.3270 mL | |
| 50 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0616 mL | |
| 60 mM | 0.0354 mL | 0.1769 mL | 0.3539 mL | 0.8847 mL | |
| 80 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6635 mL | |
| 100 mM | 0.0212 mL | 0.1062 mL | 0.2123 mL | 0.5308 mL |
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