BM0031

BMS-763534

≥98% (HPLC)

• Synonym(e): 5-Chloro-1-[(1S)-1-cyclopropyl-2-methoxyethyl]-3-[[6-(difluoromethoxy)-2,5-dimethyl-3-pyridinyl]amino]-2(1H)-pyrazinone
• Empirische Formel (Hill-System): C₁₈H₂₁ClF₂N₄O₃
• CAS-Nummer: 1188407-40-0
• Molekulargewicht: 414.83
• MDL-Nummer: MFCD30718578
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Optische Aktivität: [α]/D -40 to -55°, c = 0.8 in chloroform-d
• Farbe: white to beige
• Löslichkeit: DMSO: 25 mg/mL, clear
• Lagertemp.: room temp
• SMILES String: O=C1C(NC2=CC(C)=C(OC(F)F)N=C2C)=NC(Cl)=CN1[C@H](COC)C3CC3

Beschreibung

Biochem./physiol. Wirkung

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.).

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).

Leistungsmerkmale und Vorteile

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

Rechtliche Hinweise

Sold for research purposes only under agreement from BMS.

Sicherheitshinweise

• Lagerklassenschlüssel: 13 - Non Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable