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R121919

Chemical Structure : R121919

CAS No.: 195055-03-9

R121919 (R 121919, NBI30775)

Catalog No.: PC-21280Not For Human Use, Lab Use Only.

R121919 (NBI30775) is a highly potent, selective and nonpeptide antagonist of corticotropin-releasing factor 1 (CRF1) receptor with binding Ki of 3 nM (human and rat CRHR1), inhibits CRHR1-mediated signal transduction in transfected cells with IC50 of 60 nM.

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Biological Activity

R121919 (NBI30775) is a highly potent, selective and nonpeptide antagonist of corticotropin-releasing factor 1 (CRF1) receptor with binding Ki of 3 nM (human and rat CRHR1), inhibits CRHR1-mediated signal transduction in transfected cells with IC50 of 60 nM.
R121919 has a 1000-fold lower affinity to 70 other central receptors tested.
R121919 dose-dependently suppresses CRH-induced ACTH secretion in rat corticotrope cells.
R121919 attenuates the behavioral and endocrine responses to stress in rats.

Physicochemical Properties

M.Wt 380.54
Formula C22H32N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[6-(dimethylamino)-4-methyl-pyrid-3-yl]-2,5-dimethyl-N,N-dipropyl-pyrazolo[2,3-a]pyrimidin-7-amine

References

1. Gutman DA, et al. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80.

2. Lancel M, et al. J Psychiatr Res. 2002 Jul-Aug;36(4):197-208.

3. M E Keck, et al. Eur J Neurosci. 2001 Jan;13(2):373-80.

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