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化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D +16 to +21°, c = 0.4 in chloroform-d
顏色
white to light brown
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
room temp
SMILES 字串
ClC1=CC(OC(F)F)=CC(Cl)=C1NC2=NC(Cl)=CN([C@@H](C)C3CC3)C2=O
生化／生理作用
BMS-665053 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 </= 1.0 nM against 150 pM ovine CRF for binding human and rat CRF-R1), potency (IC50 = 4.9 nM against 1 nM CRF-stimulated cAMP production in human Y-79 retinoblastoma cells), and selectivity, displaying no affinity toward CRF-R2/CRF2 (IC50 >10 μM against 150 pM ovine CRF in binding assay). BMS-665053 exhibits anxiolytic efficacy in a defensive withdrawal anxiety test in rats in vivo (10 mg/kg p.o.) with good oral bioavailability (F = 52%).
BMS-665053 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).
特點和優勢
BMS-665053 is available through a partnership with Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.
法律資訊
Sold for research purposes only under agreement from BMS.
儲存類別代碼
13 - Non Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Xiaoliang Zhuo et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(1), 5-15 (2009-10-17)
(S)-5-Chloro-1-(1-cyclopropylethyl)-3-(2,6-dichloro-4-(trifluoromethyl)phenylamino)pyrazin-2(1H)-one (BMS-665053), a pyrazinone-containing compound, is a potent and selective antagonist of corticotropin-releasing factor receptor-1 (CRF-R1) that showed efficacy in the defensive withdrawal model for anxiety in rats, suggesting its use as a potential treatment for anxiety and depression. In
Richard A Hartz et al.
Journal of medicinal chemistry, 52(14), 4161-4172 (2009-06-26)
A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropin-releasing factor-1 (CRF(1)) receptor antagonists. Selected compounds proved efficacious in an anxiety model in rats; however, pharmacokinetic properties were not optimal. In this article, we describe an in
William D Schmitz et al.
Bioorganic & medicinal chemistry letters, 20(12), 3579-3583 (2010-05-21)
A series of 5-arylamino-1,2,4-triazin-6(1H)-ones was synthesized and evaluated as antagonists at the corticotropin releasing factor receptor. Formation of CYP-mediated oxidative reactive metabolites previously observed in a related N(3)-phenylpyrazinone structure was minimized by incorporation of the additional ring nitrogen found in
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