A-803467

目录号: HY-11079 纯度: 99.09%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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A-803467 Chemical Structure

CAS No. : 944261-79-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥594	In-stock
1 mg	￥168	In-stock
5 mg	￥337	In-stock
10 mg	￥540	In-stock
50 mg	￥1840	In-stock
100 mg	￥2960	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 2 篇科研文献

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

生物活性
纯度 & 产品资料
参考文献

生物活性

A-803467 is a potent and selective tetrodotoxin-resistant Na_v1.8 sodium channel blocker (IC₅₀=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter^[1]^[2].

IC₅₀ & Target^[1]^[2]

Na_v1.8

8 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	> 30 μM Compound: 27	Inhibition of hERG potassium channel expressed in CHO cells by isotope efflux assay Inhibition of hERG potassium channel expressed in CHO cells by isotope efflux assay	[PMID: 18176998]
HEK293	IC₅₀	0.008 μM Compound: A-803467	Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assay Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assay	[PMID: 20965738]
HEK293	IC₅₀	0.008 μM Compound: A-803467	Inhibition of human Nav1.8 channel expressed in HEK293 cells at -40 mV by patch clamp method Inhibition of human Nav1.8 channel expressed in HEK293 cells at -40 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	0.079 μM Compound: A-803467	Inhibition of human Nav1.8 channel expressed in HEK293 cells at -100 mV by patch clamp method Inhibition of human Nav1.8 channel expressed in HEK293 cells at -100 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	0.85 μM Compound: A-803467	Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay Inhibition of mouse NaV1.8 expressed in HEK293 cells by isotopic efflux assay	[PMID: 20965738]
HEK293	IC₅₀	0.85 μM Compound: 27	Inhibition of mouse recombinant Nav 1.8 channel expressed in HEK293 cells by isotopic efflux assay Inhibition of mouse recombinant Nav 1.8 channel expressed in HEK293 cells by isotopic efflux assay	[PMID: 18176998]
HEK293	IC₅₀	11.76 μM Compound: A-803467	Inhibition of human Nav1.3 channel expressed in HEK293 cells at -120 mV by patch clamp method Inhibition of human Nav1.3 channel expressed in HEK293 cells at -120 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	2.45 μM Compound: A-803467	Inhibition of human Nav1.3 channel expressed in HEK293 cells at -60 mV by patch clamp method Inhibition of human Nav1.3 channel expressed in HEK293 cells at -60 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	32.82 μM Compound: A-803467	Inhibition of human Nav1.5 channel expressed in HEK293 cells at -150 mV by patch clamp method Inhibition of human Nav1.5 channel expressed in HEK293 cells at -150 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	35.34 μM Compound: A-803467	Inhibition of human Nav1.7 channel expressed in HEK293 cells at -120 mV by patch clamp method Inhibition of human Nav1.7 channel expressed in HEK293 cells at -120 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	6.74 μM Compound: A-803467	Inhibition of human Nav1.7 channel expressed in HEK293 cells at -60 mV by patch clamp method Inhibition of human Nav1.7 channel expressed in HEK293 cells at -60 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	7.34 μM Compound: A-803467	Inhibition of human Nav1.5 channel expressed in HEK293 cells at -90 mV by patch clamp method Inhibition of human Nav1.5 channel expressed in HEK293 cells at -90 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	7.38 μM Compound: A-803467	Inhibition of human Nav1.2 channel expressed in HEK293 cells at -60 mV by patch clamp method Inhibition of human Nav1.2 channel expressed in HEK293 cells at -60 mV by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	8 nM Compound: A-803467	Inhibition of human Nav1.8 channel expressed in human HEK293 cells by patch clamp method Inhibition of human Nav1.8 channel expressed in human HEK293 cells by patch clamp method	[PMID: 17483457]
HEK293	IC₅₀	9.49 μM Compound: A-803467	Inhibition of human Nav1.2 channel expressed in HEK293 cells at -120 mV by patch clamp method Inhibition of human Nav1.2 channel expressed in HEK293 cells at -120 mV by patch clamp method	[PMID: 17483457]

体外研究
(In Vitro)

A-803467 选择性且显著地逆转 ABCG2 介导的多药耐药性。A-803467 (7.5 μM) 显著增加 ABCG2 转染细胞系中 Mitoxantrone (HY-13502) 和 Topotecan (HY-13768) 的细胞毒性。A-803467 (7.5 μM) 显著增强 ABCG2 转染细胞的细胞内 [³H]-MX 积累。A-803467 (7.5 μM；0~120 分钟) 显著阻断 ABCG2 转染细胞在不同时间段的细胞内 [³H]-MX 流出。A-803467 刺激 ABCG2 的 ATPase 活性^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

A-803467 (35 mg/kg；口服) 对雄性 NCR 裸鼠没有显著毒性^[1]。
A-803467 与 Topotecan 联合使用，显著降低植入 ABCG2 过表达 H460/MX20 细胞的小鼠的肿瘤生长。A-803467 有效恢复过表达 ABCG2 转运蛋白的肿瘤对 Topotecan 的敏感性，而对缺乏 ABCG2 表达的肿瘤没有任何显著影响^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice^[1]
Dosage:	35 mg/kg
Administration:	P.o.
Result:	Showed no noticeable toxicity in the male NCR nude mice.

分子量

357.79

Formula

C₁₉H₁₆ClNO₄

CAS 号

944261-79-4

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (139.75 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7949 mL	13.9747 mL	27.9494 mL
5 mM	0.5590 mL	2.7949 mL	5.5899 mL
10 mM	0.2795 mL	1.3975 mL	2.7949 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.99 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.99 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.09%

选择批次：

Data Sheet (642 KB) SDS (393 KB)

COA (284 KB) LCMS (277 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Anreddy N, et al. A-803467, a tetrodotoxin-resistant sodium channel blocker, modulates ABCG2-mediated MDR in vitro and in vivo. Oncotarget. 2015;6(36):39276-39291. [Content Brief]

[2]. Jarvis MF, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 2007;104(20):8520-8525. [Content Brief]

A-803467 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7949 mL	13.9747 mL	27.9494 mL	69.8734 mL
	5 mM	0.5590 mL	2.7949 mL	5.5899 mL	13.9747 mL
	10 mM	0.2795 mL	1.3975 mL	2.7949 mL	6.9873 mL
	15 mM	0.1863 mL	0.9316 mL	1.8633 mL	4.6582 mL
	20 mM	0.1397 mL	0.6987 mL	1.3975 mL	3.4937 mL
	25 mM	0.1118 mL	0.5590 mL	1.1180 mL	2.7949 mL
	30 mM	0.0932 mL	0.4658 mL	0.9316 mL	2.3291 mL
	40 mM	0.0699 mL	0.3494 mL	0.6987 mL	1.7468 mL
	50 mM	0.0559 mL	0.2795 mL	0.5590 mL	1.3975 mL
	60 mM	0.0466 mL	0.2329 mL	0.4658 mL	1.1646 mL
	80 mM	0.0349 mL	0.1747 mL	0.3494 mL	0.8734 mL
	100 mM	0.0279 mL	0.1397 mL	0.2795 mL	0.6987 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-803467944261-79-4A803467A 803467Sodium ChannelNa channelsNa+ channelspotentselectivetetrodotoxin-resistantNav1.8sodiumchannelanti-nociceptionneuropathicinflammatoryInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

A-803467

Customer Review

MCE 顾客使用本产品发表的 2 篇科研文献