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Cat. No.: HY-182965

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Glucocorticoid receptor antagonist-1

Glucocorticoid receptor antagonist-1 is an orally active glucocorticoid receptor (GR) antagonist with an IC₅₀ of 27 nM and a K_i value of 32 nM, and it exhibits low agonist activity. Glucocorticoid receptor antagonist-1 shows moderate inhibitory effects on CYP2C9 and CYP2D6, and potent inhibitory effect on CYP2C8. Glucocorticoid receptor antagonist-1 prevents Olanzapine (HY-14541)-induced weight gain in female rats. Glucocorticoid receptor antagonist-1 can be used in studies related to weight gain.

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

CAS No.: 2756355-59-4
Formula: C₃₂H₂₈FN₃O
Molecular Weight:489.58

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Glucocorticoid receptor antagonist-1 Chemical Structure

CAS No.: 2756355-59-4

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Cytochrome P450 Isoforms :

In Vitro

Glucocorticoid receptor antagonist-1 (Compound 33) inhibits GR-mediated TAT activity in human HepG2 cells with a K_i of 29 nM^[1].

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

Parmacokinetics

Species	Dose	Route	Clearance (CL)	T_1/2 (Elimination)	AUC	C_max	Bioavailability	AUC_0-∞	T_max
Rat^[1]	30 mg/kg	p.o.	/	/	/	543 ng/mL	/	7232 ng·h/mL	8 h
Monkey^[1]	20 mg/kg	p.o.	/	/	1681 ng·h/mL	176 ng/mL	8.4 %	/	/
Monkey^[1]	1 mg/kg	i.v.	16.3 mL/min/kg	5.47 h	/	/	/	/	/

In Vivo

Glucocorticoid receptor antagonist-1 (Compound 33) (10 mg/kg; p.o.; twice daily; 14 days) effectively prevents olanzapine-induced weight gain in female Sprague-Dawley rats^[1].

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

Animal Model:

Sprague-Dawley (female, olanzapine-induced weight gain model)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; twice daily; 14 days
Result:

Prevented olanzapine-induced weight gain.
Showed no decrease in plasma insulin levels.

Chemical Information

CAS No. 2756355-59-4
Molecular Weight 489.58
Formula C₃₂H₂₈FN₃O
SMILES

O=C(N1CC(C2=CC3=C(N(C4=CC=C(F)C=C4)N=C3)C=C2C)(CC5=CC=CC=C5)CC1)C6=CC=CC=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Duffy LA, et al. Development of Structurally Simplified, Non-azadecalin Glucocorticoid Antagonists which Demonstrate In Vivo Activity. Journal of medicinal chemistry. 2026 Apr 23;69(8):9104-9124. [Content Brief]

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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.

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Glucocorticoid receptor antagonist-1

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Glucocorticoid receptor antagonist-1

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Glucocorticoid receptor antagonist-1 Related Classifications

HY-182965 Related Classifications

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