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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $89 | In Stock | |
10 mg | $143 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $488 | In Stock | |
100 mg | $783 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
Description | R121919 (NBI30775) is a potent small molecule antagonist of the adrenocorticotropic hormone-releasing factor receptor 1 (CRF1), demonstrating antidepressant and anxiolytic activity, and inhibiting the CRF1 receptor, CRF2 receptor, and CRF-binding proteins. |
Targets&IC50 | CRF1 receptor:2-5 nM (Ki) |
In vitro | R121919 is a potent small-molecule CRF1 receptor antagonist, exhibiting high affinity for the CRF1 receptor with a Ki value in the range of 2–5 nM. Notably, its activity at the CRF2 receptor, CRF-binding protein, and 70 other receptor types is over 1000-fold weaker[2]. |
In vivo | In rats, R121919 demonstrates a dose-dependent reduction in adrenocorticotropic hormone and corticosterone responses to restraint stress. At a dose of 10 mg/kg R121919, peak plasma concentrations of adrenocorticotropic hormone and corticosterone are decreased by 9% and 25%, respectively[2]. Moreover, R121919 exhibits anxiolytic effects in mice with a steep dose-response curve, leading to reduced anxiety levels. Some of the intracellular targets of the drug include molecules like GR (glucocorticoid receptor), MR (mineralocorticoid receptor), BAG-1 (Bcl-2-associated athanogene-1), and AP-1 (activator protein 1)[1]. |
Alias | NBI30775 |
Molecular Weight | 380.53 |
Formula | C22H32N6 |
Cas No. | 195055-03-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 5 mg/mL (13.14 mM), Sonication is recommended. Ethanol: 80 mg/mL (210.23 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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