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BM0031

Sigma-Aldrich

BMS-763534

≥98% (HPLC)

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C18H21ClF2N4O3
Número de CAS:
1188407-40-0
Peso molecular:
414.83
MDL number:
MFCD30718578
UNSPSC Code:
12352200
NACRES:
NA.77

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.).

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.

Storage Class

13 - Non Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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
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.
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

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