Glucocorticoid receptor agonist

Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.IC50 value:Target:

Product information

CAS Number: 1245526-82-2

Molecular Weight: 396.38

Formula: C20H20F4N2O2

Synonym:

1H-Pyrrolo[2,3-c]pyridine-2-ethanol, α-[2-(5-fluoro-2-hydroxyphenyl)-2-methylpropyl]-α-(trifluoromethyl)-, (αR)-

Chemical Name: 4-fluoro-2-[(4R)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-({1H-pyrrolo[2,3-c]pyridin-2-yl}methyl)pentan-2-yl]phenol

Smiles: CC(C)(C[C@@](O)(CC1=CC2=CC=NC=C2N1)C(F)(F)F)C1=CC(F)=CC=C1O

InChiKey: JFUAWXPBHXKZGA-IBGZPJMESA-N

InChi: InChI=1S/C20H20F4N2O2/c1-18(2,15-8-13(21)3-4-17(15)27)11-19(28,20(22,23)24)9-14-7-12-5-6-25-10-16(12)26-14/h3-8,10,26-28H,9,11H2,1-2H3/t19-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL (252.28 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

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.

Products are for research use only. Not for human use.