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BM0031 Sigma-Aldrich

BMS-763534

≥98% (HPLC)

Synonym: 5-Chloro-1-[(1S)-1-cyclopropyl-2-methoxyethyl]-3-[[6-(difluoromethoxy)-2,5-dimethyl-3-pyridinyl]amino]-2(1H)-pyrazinone

  • CAS Number 1188407-40-0

  • Empirical Formula (Hill Notation) C18H21ClF2N4O3

  • Molecular Weight 414.83

  •  MDL number MFCD30718578

  •  NACRES NA.77

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Properties

Related Categories B, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
optical activity   [α]/D -40 to -55°, c = 0.8 in chloroform-d
color   white to beige
solubility   DMSO: 25 mg/mL, clear
storage temp.   room temp
SMILES string   O=C1C(NC2=CC(C)=C(OC(F)F)N=C2C)=NC(Cl)=CN1[C@H](COC)C3CC3

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

BMS-763534 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 = 0.26 & 0.4 nM against 150 pM ovine CRF for binding rat & human CRF-R1, respectively), potency (IC50 = 1.0 nM against 0.3 nM CRF-stimulated ATCH secretion from primary rat anterior pituitary cells), and selectivity, displaying little affinity toward porcine CRF-R2/CRF2 and 46 other receptor/channel/transporter proteins (IC50 >10 μM). BMS-763534 inhibits CRF-stimulated cAMP production in human Y-79 retinoblastoma cells in cultures (pA2 = 9.47) and exhibits anxiolytic efficacy in a rat situational anxiety model in vivo (0.5-3 mg/kg p.o.).

Features and Benefits

BMS-763534 is available through a partnership with Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.

Legal Information

Sold for research purposes only under agreement from BMS.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis (COA)

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Protocols & Articles

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Peer-Reviewed Papers
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References

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