| Identification | Back Directory | [Name]
BMS-763534 | [CAS]
1188407-40-0 | [Synonyms]
BMS-763534
BMS-763534 >=98% (HPLC)
2(1H)-Pyrazinone, 5-chloro-1-[(1S)-1-cyclopropyl-2-methoxyethyl]-3-[[6-(difluoromethoxy)-2,5-dimethyl-3-pyridinyl]amino]- | [Molecular Formula]
C18H21ClF2N4O3 | [MDL Number]
MFCD30718578 | [MOL File]
1188407-40-0.mol | [Molecular Weight]
414.83 |
| Chemical Properties | Back Directory | [Melting point ]
103.4-104.4 °C(Solv: heptane (142-82-5)) | [Boiling point ]
470.4±55.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: 25mg/mL, clear | [form ]
powder | [pka]
1.89±0.40(Predicted) | [color ]
white to beige | [Optical Rotation]
[α]/D -40 to -55°, c = 0.8 in chloroform-d | [SMILES]
O=C1C(NC2=CC(C)=C(OC(F)F)N=C2C)=NC(Cl)=CN1[C@H](COC)C3CC3 |
| Hazard Information | Back Directory | [Uses]
BMS-763534 is a CRF1 antagonist that inhibits neurological disorders such as depression and anxiety.[1]. | [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.). | [References]
[1] Development of an Efficient Synthesis of Two CRF Antagonists for the Treatment of Neurological Disorders |
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