R 121919 hydrochloride

Name: R 121919 hydrochloride
Brand: Tocris Bioscience
SKU: 6530

Tocris Bioscience, part of Bio-Techne | Catalog # 6530

COA / SDS

High affinity CRF1 antagonist; orally bioavailable

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Technical Data
Citations

Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

High affinity CRF1 antagonist; orally bioavailable

View all CRF1 Receptor Antagonists »

Product Description

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

Product Specifications

Molecular Weight

416.99

Formula

C₂₂H₃₂N₆.HCl

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine hydrochloride

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.

Solubility

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

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 all affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.40 mL	11.99 mL	23.98 mL
5 mM	0.48 mL	2.40 mL	4.80 mL
10 mM	0.24 mL	1.20 mL	2.40 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Calculators

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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Background References

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

Heinrichs Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 2002 PMID: 12093593
Jutkiewicz 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). 2005 PMID: 15696320
Gutman The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 2003 PMID: 12538845
Chen and Grigoriadis 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.