Cat. No.: HY-151876

Glucocorticoid receptor modulator 1

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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.

For research use only. We do not sell to patients.

Purity: 99.79%
CAS No.: 2868357-11-1
Formula: C₂₄H₂₃ClN₂O₄S
Molecular Weight:470.97

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)

Glucocorticoid receptor modulator 1 Chemical Structure

CAS No.: 2868357-11-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC₅₀: 9 nM (NF-κB), 130 nM (AP-1)^[1]

All NF-κB Isoforms :

All AP-1 Isoforms :

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.

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.

Chemical Information

CAS No. 2868357-11-1
Appearance Solid
Molecular Weight 470.97
Formula C₂₄H₂₃ClN₂O₄S
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1233 mL

10.6164 mL

21.2328 mL

5 mM

0.4247 mL

2.1233 mL

4.2466 mL

10 mM

0.2123 mL

1.0616 mL

2.1233 mL

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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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li D, Hou T, et al. Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators. J Med Chem. 2022 Nov 18. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Glucocorticoid receptor modulator 1

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Glucocorticoid receptor modulator 1

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

MCE Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All NF-κB Isoforms

All AP-1 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Glucocorticoid receptor modulator 1 Related Classifications

HY-151876 Related Classifications