Pexacerfont - ≥98%(HPLC), high purity , Corticotropin releasing factor receptor 1 antagonist, CAS No.459856-18-9, Corticotropin releasing factor receptor 1 antagonist

Item Number
P287633
Grouped product items
SKUSizeAvailabilityPrice Qty
P287633-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$197.90
P287633-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$781.90

Potent and selective CRF1antagonist; anxiolytic

View related series
CRF1 receptor Antagonist

Basic Description

SynonymsD70085 | D10022 | LF1VBG4ZUK | Pexacerfont [USAN:INN] | ZB1563 | AKOS004115453 | BMS 562086 | EX-A3079 | AKOS040742389 | CRF1 ANTAGONIST | PEXACERFONT | CS-6630 | PEXACERFONT [INN] | 8-(6-Methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]p
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent and selective corticotropin-releasing factor 1 receptor (CRF1) antagonist (IC50= 6.1 nM). Displays >150 fold selectivity for CRF1over CRF2b. Inhibits CRF-mediated adrenocorticotropic hormone (ACTH) release from pituitary cell culture (IC50= 129 nM)
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionCorticotropin releasing factor receptor 1 antagonist

Product Properties

ALogP3.8

Associated Targets(Human)

CRHR1 Tclin Corticotropin-releasing factor receptor 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CRHR1 Tclin Corticotropin releasing factor receptor 1 (2996 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TACR2 Tchem Neurokinin 2 receptor (3341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CRHR2 Tchem Corticotropin releasing factor receptor 2 (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CRHBP Tbio Corticotropin-releasing factor-binding protein (6 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Pan troglodytes (415 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Serum (58 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsome (341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[(2R)-butan-2-yl]-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
INCHI InChI=1S/C18H24N6O/c1-7-10(2)19-18-22-13(5)21-17-16(12(4)23-24(17)18)14-8-9-15(25-6)20-11(14)3/h8-10H,7H2,1-6H3,(H,19,21,22)/t10-/m1/s1
InChi Key LBWQSAZEYIZZCE-SNVBAGLBSA-N
Canonical SMILES CCC(C)NC1=NC(=NC2=C(C(=NN21)C)C3=C(N=C(C=C3)OC)C)C
Isomeric SMILES CC[C@@H](C)NC1=NC(=NC2=C(C(=NN21)C)C3=C(N=C(C=C3)OC)C)C
PubChem CID 9884366
Molecular Weight 340.43

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 34.04, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 34.04, Max Conc. mM: 100

Related Documents

References

1. Mochizuki M, Kojima T, Kobayashi K, Kotani E, Ishichi Y, Kanzaki N, Nakagawa H, Okuda T, Kosugi Y, Yano T et al..  (2017)  Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF1 receptor antagonist..  Bioorg Med Chem,  25  (5): (1556-1570).  [PMID:28174066]

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