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R121919

Catalog No. T16713 CAS 195055-03-9

Synonyms: NBI30775

R121919 (NBI30775) is a potent small molecule adrenocorticotropic hormone-releasing factor receptor 1 (CRF1) receptor antagonist with antidepressant and anxiolytic activity that inhibits the CRF1 receptor, the CRF2 receptor, and the CRF-binding proteins.

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R121919, CAS 195055-03-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 89.00
10 mg	In stock	$ 143.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 488.00
100 mg	In stock	$ 783.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.75%

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Description	R121919 (NBI30775) is a potent small molecule adrenocorticotropic hormone-releasing factor receptor 1 (CRF1) receptor antagonist with antidepressant and anxiolytic activity that inhibits the CRF1 receptor, the CRF2 receptor, and the 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].

Synonyms	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

Solubility Information

DMSO: 5 mg/mL(13.14 mM), Sonication is recommended.

Ethanol: 80 mg/mL(210.23 mM), Sonication is recommended.

References and Literature

1. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8. 2. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

R121919 195055-03-9 Others R-121919 NBI30775 NBI-30775 R 121919 NBI 30775 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.