RPT193 是具有口服活性的CCR4抑制剂。RPT193 抑制 Th2 炎性免疫细胞募集到炎症组织,在特应性皮炎、哮喘等疾病中起着过敏性炎症的具有重要作用。
产品描述
RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research [1].
体外活性
RPT193 (1 nM-10 μM) inhibits Th2 cells chemotaxis or migration with IC 50 s of ~370 nM [2].
体内活性
RPT193 (100 mg/kg; p.o.; once daily; 2 d, 1 d before OVA-challenge) reduces skin inflammation in an acute ovalbumin (OVA)-induced atopic dermatitis model in mice [2]. Animal Model: Acute ovalbumin (OVA)-induced atopic dermatitis model in mouse [2] Dosage: 100 mg/kg Administration: Oral gavage; once daily; for 2 days, started 1 day before OVA-challenge (in mouse ear) Result: Decreased the ear thickness significantly.
Cas No.
2366152-15-8
分子式
C27H34Cl3N5O2
分子量
566.95
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years