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经验公式(希尔记法):
C11H9Cl2N3O3S
化学文摘社编号:
分子量:
334.18
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
InChI key
FLSMVCMSUNISFK-UHFFFAOYSA-N
SMILES string
O=S(C1=CC=CC(Cl)=C1Cl)(NC2=NC=CN=C2OC)=O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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