| 描述 |
RPT193是CCR4的口服活性抑制剂,阻止Th2炎症免疫细胞向炎症组织的募集。RPT193可用于过敏性皮炎、哮喘和其他疾病的过敏性炎症研究[1]。
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| 相关类别 |
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| 靶点 |
CCR4
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| 体外研究 |
RPT193(1 nM-10μM)抑制Th2细胞的趋化性或迁移,IC50s约为370 nM[2]。
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| 体内研究 |
RPT193(100 mg/kg；p.o.；每日一次；OVA激发前2天、1天)可降低小鼠急性卵清蛋白(OVA)诱导的特应性皮炎模型的皮肤炎症[2]。动物模型：小鼠急性卵清蛋白(OVA)诱导的特应性皮炎模型[2]剂量：100 mg/kg灌胃；每天一次；连续2天,在OVA激发前1天开始(小鼠耳)。结果：耳壁厚度显著降低。
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| 参考文献 |
[1]. Bissonnette R, et al. RPT193, an oral CCR4 inhibitor: Efficacy results from a randomized, placebo-controlled Phase 1b monotherapy trial in patients with moderate-to-severe atopic dermatitis[C]//EXPERIMENTAL DERMATOLOGY. 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY, 2021, 30: 40-41. [2]. Cheng L, et al. Development and first-in-human characterization of a potent oral CCR4 antagonist for the treatment of atopic dermatitis[C]//Journal of Investigative Dermatology. STE 800, 230 PARK AVE, NEW YORK, NY 10169 USA: ELSEVIER SCIENCE INC, 2020, 140(7): S77-S77.
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