Pexacerfont

Pricing Availability   Qty
Cat.No. 6451 - Pexacerfont | C18H24N6O | CAS No. 459856-18-9
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective corticotropin-releasing factor 1 receptor (CRF1) antagonist (IC50 = 6.1 nM). Displays >150 fold selectivity for CRF1 over CRF2b. Inhibits CRF-mediated adrenocorticotropic hormone (ACTH) release from pituitary cell culture (IC50 = 129 nM). Displays anxiolytic effects in rat behavioral paradigms.

Technical Data

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 Data

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

Preparing Stock Solutions

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

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

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References

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

Gilligan et al (2009) 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. 52 3084 PMID: 19361209


If you know of a relevant reference for Pexacerfont, please let us know.

View Related Products by Target

View Related Products by Product Action

View all CRF1 Receptor Antagonists

Keywords: Pexacerfont, Pexacerfont supplier, BMS, 562086, BMS562086, corticotrophin, releasing, hormone, receptor, 1, antagonists, antagonism, CRF1, anxiolytic, Receptors, 6451, Tocris Bioscience

Citations for Pexacerfont

Citations are publications that use Tocris products.

Currently there are no citations for Pexacerfont. Do you know of a great paper that uses Pexacerfont from Tocris? Please let us know.

Reviews for Pexacerfont

There are currently no reviews for this product. Be the first to review Pexacerfont and earn rewards!

Have you used Pexacerfont?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

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

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:

  • Anterior Pituitary Regulation
  • Blood Pressure Regulation
  • Feeding and Appetite Regulation
  • Glucose Regulation
  • Peptide Hormone Processing
Depression

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.