R 121919 hydrochloride

Pricing Availability   Qty
Description: High affinity CRF1 antagonist; orally bioavailable
Chemical Name: 3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine hydrochloride
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for R 121919 hydrochloride

R 121919 hydrochloride is a high affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable.

Technical Data for R 121919 hydrochloride

M. Wt 416.99
Formula C22H32N6.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 195055-66-4
PubChem ID 22029352
Smiles CCCN(C1=CC(C)=NC2=C(C3=CN=C(N(C)C)C=C3C)C(C)=NN12)CCC.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for R 121919 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 41.7 100
DMSO 4.17 10 with gentle warming

Preparing Stock Solutions for R 121919 hydrochloride

The following data is based on the product molecular weight 416.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.4 mL 11.99 mL 23.98 mL
5 mM 0.48 mL 2.4 mL 4.8 mL
10 mM 0.24 mL 1.2 mL 2.4 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets for R 121919 hydrochloride

References for R 121919 hydrochloride

References are publications that support the biological activity of the product.

Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216

Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 180 215 PMID: 15696320

Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID: 12538845

Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID: 12093593

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Citations for R 121919 hydrochloride

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.