A-803467

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

A-803467 是一种强效、选择性的河豚毒素不敏感型 Nav1.8 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。

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

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.

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. Animal Model:Nude miceDosage:35 mg/kg Administration:P.o.Result:Showed no noticeable toxicity in the male NCR nude mice.

A-803467 | A 803467 | A803467

Membrane Transporter/Ion Channel

Sodium Channel

Na(V1.8) channel

Neurological Disease

——

944261-79-4

357.79

C19H16ClNO4

>98% (HPLC)

Ethanol: 11 mg/mL (30.74 mM); DMSO: 72 mg/mL (201.23 mM)

O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)NC3=CC(OC)=CC(OC)=C3

5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide

(-20℃)

With Ice Pack

≥ 2 years