1245526-82-2

1245526-82-2 structure

Name: Glucocorticoid receptor agonist
Chemical Name: 4-fluoro-2-[(4R)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol
CAS Number: 1245526-82-2
Molecular Formula: C₂₀H₂₀F₄N₂O₂
Molecular Weight: 396.37900
Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
Create Date: 2018-11-27 21:01:53
Modify Date: 2025-08-26 15:34:29
Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.IC50 value:Target:

Name	4-fluoro-2-[(4R)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1H-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol
Synonyms	Glucocorticoid receptor agonist CS-0520

Description	Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.IC50 value:Target:
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor Research Areas >> Metabolic Disease
Animal Admin	Animal administration [1]Female Balb/c mice weighing approximately 20 g were used. Mice were administered the test compound and in Cremophor (po) approximately 60 min prior to LPS/D-gal administration. The volume of oral gavage was 0.15 mL. Then mice were administered LPS (E. coli LPS 055:85, 1.0 μg/mouse) plus D-gal (50 mg/kg) intravenously in 0.2 mL of pyrogen-free saline. One hour after LPS/D-gal, each mouse was anesthetized, bled by cardiac puncture, and collected for serum TNF-R and compound levels. Blood samples were centrifuged at 2500 rpm for 10-15 min, the serum was decanted, and samples were stored frozen at -70°C until transfer either for TNF-R determination or to Drug Metabolism and Pharmacokinetics for plasma concentration analysis by HPLC. The concentration of TNF-R in the serum was measured by a commercially available ELISA kit. ELISA was performed. All samples are assayed in duplicate.
References	[1]. Riether, Doris et al.Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. Journal of Medicinal Chemistry (2010), 53(18), 6681-6698.