BI-6901 是一种有效的选择性CCR10 拮抗剂 (pIC50=9.0)。BI-6901 对其他 GPCRs 表现出高选择性，包括许多其他趋化因子受体。BI-6901 对接触性超敏小鼠 DNFB 模型有效，可用于炎症研究。
BI 6901 is a potent, selective CCR10 antagonist (pIC50=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research[1].
BI-6901 (intraperitoneal injection; 100 mg/kg; bid.) exhibits a dose-dependent anti-inflammatory response against DNFB stimulated ear swelling in sensitized mice. The level of efficacy observed for BI-6901 is similar to that observed with anti-CCL27 antibody in the same model (60-85%)[1].
[1]. Asitha Abeywardane, et al. N-Arylsulfonyl-α-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5277-5283.
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