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A-803467

CAS No. : 944261-79-4

MCE 国际站：A-803467

产品活性：A-803467 是一种强效、选择性的河豚毒素不敏感型 Na_v1.8 钠通道阻断剂 (IC₅₀=8 nM)。A-803467 在神经性疼痛和炎症性疼痛模型中有缓解疼痛作用。A-803467 通过与 ATP-binding cassette subfamily G member 2 (ABCG2) 转运蛋白的相互作用，增强了传统抗癌物的化疗敏感性。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

In Vitro: A-803467 selectively and significantly reverses the ABCG2-mediated multidrug resistance. A-803467 (7.5 μM) significantly increases the cytotoxicity of mitoxantrone and topotecan in ABCG2-transfected cell lines. A-803467 (7.5 μM) significantly enhanced theintracellular [³H]-MX accumulation in ABCG2-transfected cells. A-803467 (7.5 μM; 0~120 minutes) significantly blocks the intracellular [³H]-MX efflux at different time periods from ABCG2-transfected cells. A-803467 stimulates the ATPase activity of ABCG2.

In Vivo: A-803467 (35 mg/kg; p.o.) shows no noticeable toxicity in the male NCR nude mice.
A-803467 in combination with topotecan, significantly decreases the tumor growth in mice implanted with ABCG2 overexpressing H460/MX20 cells. A-803467 effectively restores the sensitivity of tumors overexpressing ABCG2 transporter to topotecan without having any significant effect on tumors lacking ABCG2 expression.

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