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  2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. A-803467

A-803467 是一種強(qiáng)效、選擇性的河豚毒素不敏感型 Nav1.8 鈉通道阻斷劑 (IC50=8 nM)。A-803467 在神經(jīng)性疼痛和炎癥性疼痛模型中有緩解疼痛作用。A-803467 通過(guò)與 ATP-binding cassette subfamily G member 2 (ABCG2) 轉(zhuǎn)運(yùn)蛋白的相互作用，增強(qiáng)了傳統(tǒng)抗癌物的化療敏感性。

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A-803467 Chemical Structure

A-803467 Chemical Structure

CAS No. : 944261-79-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
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
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200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

查看 Sodium Channel 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 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]

Nav1.8

8 nM (IC50)

細(xì)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]
體外研究
(In Vitro)

A-803467 選擇性且顯著地逆轉(zhuǎn) ABCG2 介導(dǎo)的多藥耐藥性。A-803467 (7.5 μM) 顯著增加 ABCG2 轉(zhuǎn)染細(xì)胞系中 Mitoxantrone (HY-13502) 和 Topotecan (HY-13768) 的細(xì)胞毒性。A-803467 (7.5 μM) 顯著增強(qiáng) ABCG2 轉(zhuǎn)染細(xì)胞的細(xì)胞內(nèi) [3H]-MX 積累。A-803467 (7.5 μM；0~120 分鐘) 顯著阻斷 ABCG2 轉(zhuǎn)染細(xì)胞在不同時(shí)間段的細(xì)胞內(nèi) [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.
體內(nèi)研究
(In Vivo)

A-803467 (35 mg/kg；口服) 對(duì)雄性 NCR 裸鼠沒(méi)有顯著毒性[1]。
A-803467 與 Topotecan 聯(lián)合使用，顯著降低植入 ABCG2 過(guò)表達(dá) H460/MX20 細(xì)胞的小鼠的腫瘤生長(zhǎng)。A-803467 有效恢復(fù)過(guò)表達(dá) ABCG2 轉(zhuǎn)運(yùn)蛋白的腫瘤對(duì) Topotecan 的敏感性，而對(duì)缺乏 ABCG2 表達(dá)的腫瘤沒(méi)有任何顯著影響[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 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (139.75 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.99 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.99 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.09%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱(chēng)：
A-803467
目錄號(hào)：
HY-11079
需求量：