Fortfahren mit
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
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Über diesen Artikel
Empirische Formel (Hill-System):
C18H21ClF2N4O3
CAS-Nummer:
Molekulargewicht:
414.83
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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
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.).
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).
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.
Lagerklasse
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Nicholas J Lodge et al.
Neuropharmacology, 67, 284-293 (2012-11-24)
BMS-763534 is a potent (CRF(1) IC(50) = 0.4 nM) and selective (>1000-fold selectivity vs. all other sites tested) CRF(1) receptor antagonist (pA2 = 9.47 vs. CRF(1)-mediated cAMP production in Y79 cells). BMS-763534 accelerated the dissociation of (125)I-o-CRF from rat frontal cortex membrane CRF(1) receptors consistent
Richard A Hartz et al.
Bioorganic & medicinal chemistry letters, 20(6), 1890-1894 (2010-02-24)
A series of N(3)-pyridylpyrazinones was investigated as corticotropin-releasing factor-1 receptor antagonists. It was observed that the binding affinity of analogues containing a pyridyl group was influenced not only by the substitution pattern on the pyridyl group, but also by the
Richard A Hartz et al.
Journal of medicinal chemistry, 52(23), 7653-7668 (2009-12-04)
Detailed metabolic characterization of 8, an earlier lead pyrazinone-based corticotropin-releasing factor-1 (CRF(1)) receptor antagonist, revealed that this compound formed significant levels of reactive metabolites, as measured by in vivo and in vitro biotransformation studies. This was of particular concern due
Global Trade Item Number
| SKU | GTIN |
|---|---|
| BM0031-5MG | 04061832269610 |
| BM0031-25MG | 04061832269603 |