2. Vitamin D Related/Nuclear Receptor NF-κB Immunology/Inflammation
  3. Glucocorticoid Receptor NF-κB AP-1
  4. Glucocorticoid receptor modulator 1

Glucocorticoid receptor modulator 1 

Cat. No.: HY-151876 Purity: 99.79%
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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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Glucocorticoid receptor modulator 1 Chemical Structure

Glucocorticoid receptor modulator 1 Chemical Structure

CAS No. : 2868357-11-1

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Based on 1 publication(s) in Google Scholar

Glucocorticoid receptor modulator 1 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 9 nM (NF-κB), 130 nM (AP-1)[1]
Cellular Effect
Cell Line Type Value Description References
Peritoneal macrophage IC50
6.9 μM
Compound: B-53
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
[PMID: 36399795]
Peritoneal macrophage IC50
7.74 μM
Compound: B-53
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
[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.

Glucocorticoid receptor modulator 1 Related Antibodies

RT-PCR[1]

Cell Line: Mouse macrophage RAW264.7 cells
Concentration: 10 μM
Incubation Time: 24 h
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

Glucocorticoid receptor modulator 1 (5, 10 and 20 mg/kg; p.o.; for 24 days) relieves dermatitis in mice and suppresses the expression of inflammatory factors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C mice (5 weeks; 2,4-dinitrochlorobenzene-induced atopic dermatitis model)[1]
Dosage: 5, 10 and 20 mg/kg
Administration: p.o.; for 24 days
Result: Significantly improved the skin damage in a dose-dependent manner, and suppressed inflammatory factors of IL-6, IL-1β, TSLP, and MMP-13.
Molecular Weight

470.97

Formula

C24H23ClN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=C(C=C(C(C)=C1)Cl)S(=O)(NC2=CC=C3C(CCCN3C(C4=CC=CC=C4)=O)=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1233 mL 10.6164 mL 21.2328 mL
5 mM 0.4247 mL 2.1233 mL 4.2466 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

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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Glucocorticoid receptor modulator 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Glucocorticoid receptor modulator 12868357-11-1Glucocorticoid receptor modulator1Glucocorticoid receptor modulator-1Glucocorticoid ReceptorNF-κBAP-1Nuclear factor-κBNuclear factor-kappaBActivator Protein 1anti-inflammatorydermatitisDNCBInhibitorinhibitorinhibit

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