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BM0034 Sigma-Aldrich

BMS-764459

≥98% (HPLC)

Synonym: (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, 4-[(1S)-1-Cyclopropyl-2-methoxyethyl]-6-[[6-(difluoromethoxy)-2,5-dimethyl-3-pyridinyl]amino]-4,5-dihydro-5-oxo-2-pyrazinecarbonitrile

  • CAS Number 1188407-45-5

  • Empirical Formula (Hill Notation) C19H21F2N5O3

  • Molecular Weight 405.40

  •  MDL number MFCD18642630

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Properties

Related Categories B, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
assay   ≥98% (HPLC)
form   powder
color   white to light brown
solubility   DMSO: 20 mg/mL, clear
storage temp.   room temp

Description

Packaging

5, 25 mg in glass bottle

Legal Information

Sold for research purposes only under agreement from BMS.

Biochem/physiol Actions

BMS-764459 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 = 0.86 nM against 150 pM ovine CRF for binding rat CRF-R1), potency (IC50 = 1.9 nM against 1 nM CRF-stimulated cAMP production in human Y-79 retinoblastoma cells), and selectivity, displaying little affinity toward CRF-R2/CRF2 and 43 other receptor/channel/transporter proteins (IC50 >10 μM). BMS-764459 exhibits anxiolytic efficacy in a rat defensive withdrawal model of anxiety in vivo (1-3 mg/kg p.o.) with good oral bioavailability (F in dogs = 53% with 2 mg/kg in suspension and 70% with 3 mg/kg in solution).

Features and Benefits

BMS-764459 is available through a partnership between Sigma Life Science and Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

Protocols & Articles

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Peer-Reviewed Papers
15

References

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