AZD 2098

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD2098 是一种有效的、选择性的、口服生物可利用的 CCR4 受体拮抗剂，hCCR4 的 pIC50 为 7.8，rCCR4 的 pIC50 为 8.0。

AZD2098 is a potent, selective, orally bioavailable CCR4 receptor antagonist with pIC50 of 7.8 for hCCR4, pIC50 of 8.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.3; exhibits anti-inflammatory effects in Brown-Norway rats sensitized to ovalbumin.Asthma Phase 1 Clinical.

AZD2098 potently inhibits chemokine-induced cellular responses, with pIC50 of 7.5 and 6.3 against CCL22-induced Ca2+ influx in hCCR4-expressing CHO cells and CCL17- or CCL22-induced chemotaxis of primary human Th2 cells respectively.

AZD2098 (73.5-5.0 μg/kg; p.o.; BID; twice a day; 1 hour before and every 12 hours after antigen challenge) exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats, and the changes are first visible at a dose of 0.22 μmol/kg and maximal at 7.5 μmol/kg. Animal Model:Brown-Norway rats Dosage:73.5 μg/kg, 250.6 μg/kg, 735.2 μg/kg, 1.0 mg/kg, 2.5 mg/kg, 5.0 mg/kg Administration:Oral administration; twice a day; 1 hour before and every 12 hours after antigen challenge Result:Exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats.

AZD2098 | AZD-2098

GPCR/G Protein

Chemokine Receptor

CCR4

Inflammation/Immunology

Asthma

566203-88-1

334.171

C11H9Cl2N3O3S

>98% (HPLC)

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=S(C1=CC=CC(Cl)=C1Cl)(NC2=NC=CN=C2OC)=O

2,3-Dichloro-N-(3-methoxy-2-pyrazinyl)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years