R 121919 hydrochloride

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Cat.No. 6530 - R 121919 hydrochloride | C22H32N6.HCl | CAS No. 195055-66-4
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)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

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

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

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

Preparing Stock Solutions

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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References

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

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