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Submit ReviewR 121919 hydrochloride
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)
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 |
| InChI Key | LGDDPMVPDGTXMV-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
If you know of a relevant reference for R 121919 hydrochloride, please let us know.
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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
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.