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Referencia número: 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.

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No. CAS: 2756355-59-4
Fòrmula: C₃₂H₂₈FN₃O
Peso molecular:489.58

Almacenamiento:

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

Glucocorticoid receptor antagonist-1 Chemical Structure

No. CAS: 2756355-59-4

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Use of MCE Products

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

Actividad biológica
- Descripciòn
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
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Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas Cytochrome P450 :

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

No. CAS 2756355-59-4
Peso molecular 489.58
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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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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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Glucocorticoid receptor antagonist-1

Ver todos los productos específicos de isoformas Cytochrome P450

Actividad biológica

Descripciòn

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

Glucocorticoid receptor antagonist-1 Related Classifications

HY-182965 Related Classifications

Bioz

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