Pexacerfont

Name: Pexacerfont
Brand: Tocris Bioscience
SKU: 6451

Tocris Bioscience, part of Bio-Techne | Catalog # 6451

COA / SDS

Potent and selective CRF1 antagonist; anxiolytic

Key Product Details

Description:	Potent and selective CRF₁ antagonist; anxiolytic
Chemical Name:	8-(6-Methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
Purity:	≥98% (HPLC)
Molecular Weight:	340.43

View Full Technical Details for Pexacerfont

Technical Data
Citations

Biological Activity for Pexacerfont

Pexacerfont is a potent and selective corticotropin-releasing factor 1 receptor (CRF₁) antagonist (IC₅₀ = 6.1 nM). Displays >150 fold selectivity for CRF₁ over CRF_2b. Inhibits CRF-mediated adrenocorticotropic hormone (ACTH) release from pituitary cell culture (IC₅₀ = 129 nM). Displays anxiolytic effects in rat behavioral paradigms.

Technical Data for Pexacerfont

M. Wt	340.43
Formula	C₁₈H₂₄N₆O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	459856-18-9
PubChem ID	9884366
InChi Key	LBWQSAZEYIZZCE-SNVBAGLBSA-N
Smiles	CC[C@H](NC1=NC(C)=NC2=C(C3=C(N=C(C=C3)OC)C)C(C)=NN12)C

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 for Pexacerfont

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	34.04	100
	ethanol	34.04	100

Preparing Stock Solutions for Pexacerfont

The following data is based on the product molecular weight 340.43.

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	2.94 mL	14.69 mL	29.37 mL
5 mM	0.59 mL	2.94 mL	5.87 mL
10 mM	0.29 mL	1.47 mL	2.94 mL
50 mM	0.06 mL	0.29 mL	0.59 mL

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References for Pexacerfont

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

Gilligan Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF₁) antagonists. J.Med.Chem. 2009 PMID: 19361209