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方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=S(C1=CC=CC(Cl)=C1Cl)(NC2=NC=CN=C2OC)=O
InChI key
FLSMVCMSUNISFK-UHFFFAOYSA-N
生化/生理作用
AZD-2098 is an orally active, potent and selective CCR4 antagonist (pIC50 = 7.8/8.0/8.0/7.6 against CCL22 binding to human/mouse/rat/dog CCR4; inactive toward CXCR1/2 & CCR1/2b/5/7/8 at 10 μM) with little or no activity toward a panel of ∼120 receptors/enzymes. AZD-2098 effectively inhibits chemokine-induced cellular responses in vitro (pIC50 = 7.5 against CCL22-induced calcium influx in hCCR4-expressing CHO cells; pIC50 = 6.3 against CCL17- or CCL22-induced chemotaxis of primary human Th2 cells) and exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats in vivo (Emax = 7.5 μmol/kg p.o.; 1 h before and every 12 h after antigen challenge).
Orally active, potent and selective CCR4 antagonist with efficacy against antigen-induced inflammatory response in ovalbumin-sensitized rats in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.
Nicholas Kindon et al.
ACS medicinal chemistry letters, 8(9), 981-986 (2017-09-28)
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