AM-2099

目录号: HY-100727 纯度: 98.06%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

AM-2099是电压门控钠通道Nav1.7的有效，选择性的抑制剂，对人类Nav1.7的IC₅₀值为0.16 μM。

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AM-2099 Chemical Structure

CAS No. : 1443373-17-8

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10 mM * 1 mL in DMSO	￥990	In-stock
5 mg	￥900	In-stock
10 mg	￥1500	In-stock
50 mg	￥4000	In-stock
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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
实验参考方法
纯度 & 产品资料
参考文献

生物活性

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC₅₀ of 0.16 μM for human Nav1.7.

IC₅₀ & Target

Nav1.7

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	> 30 μM Compound: 16	Inhibition of 20% inactivated human Nav1.8 expressed in CHO cells assessed as inhibition of TTX-resistant current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.8 expressed in CHO cells assessed as inhibition of TTX-resistant current by whole cell patch clamp method	[PMID: 27994738]
CHO	IC₅₀	2.1 μM Compound: 16	Inhibition of 20% inactivated human Nav1.2 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.2 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
CHO	IC₅₀	21 μM Compound: 16	Inhibition of 20% inactivated human Nav1.3 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.3 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	> 30 μM Compound: 16	Inhibition of human Nav1.5 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.5 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	> 30 μM Compound: 16	Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes measured after 90 mins by TopCount scintillation counting method Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes measured after 90 mins by TopCount scintillation counting method	[PMID: 27994738]
HEK293	IC₅₀	> 30 μM Compound: 1	Inhibition of human Nav1.5 expressed in HEK293 cells assessed as reduction in peak inward current by ionworks quattro electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells assessed as reduction in peak inward current by ionworks quattro electrophysiology assay	[PMID: 28287723]
HEK293	IC₅₀	0.009 μM Compound: 16	Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -60 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -60 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.14 μM Compound: 16	Inhibition of 20% inactivated human Nav1.7 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.7 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.16 μM Compound: 1	Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assay	[PMID: 28287723]
HEK293	IC₅₀	0.16 μM Compound: 16	Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.18 μM Compound: 16	Inhibition of 20% inactivated mouse Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated mouse Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	16 μM Compound: 16	Inhibition of 20% inactivated human Nav1.5 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.5 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	17 μM Compound: 16	Inhibition of 20% inactivated human Nav1.4 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.4 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	3.7 μM Compound: 16	Inhibition of 20% inactivated human Nav1.6 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.6 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	7.2 μM Compound: 16	Inhibition of human Nav1.7 in closed state expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -140 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.7 in closed state expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -140 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	7.3 μM Compound: 16	Inhibition of 20% inactivated human Nav1.1 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.1 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK-293T	IC₅₀	0.16 μM Compound: 16	Inhibition of 20% inactivated cynomolgus monkey Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated cynomolgus monkey Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK-293T	IC₅₀	0.18 μM Compound: 16	Inhibition of 20% inactivated dog Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated dog Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK-293T	IC₅₀	3.5 μM Compound: 16	Inhibition of 20% inactivated rat Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated rat Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]

体外研究
(In Vitro)

在异源细胞中，在人、小鼠、狗和食蟹猴 NaV1.7 中观察到类似的抑制作用，但对大鼠 NaV1.7 的活性降低。AM-2099 的选择性是 Nav1.3、Nav1.4、Nav1.5 和 Nav1.8 的 100 多倍，而对 Nav1.1、Nav1.2 和 Nav1.6 的选择性水平较低。AM-2099 对 hERG 表现出低亲和力 (>30 μM)，并且对一组 100 种激酶 (1 μM) 和广泛的 CEREP 组 (10 μM) 显示出不超过 50% 的抑制。^[1]。

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

体内研究
(In Vivo)

AM-2099 在大鼠和狗身上表现出良好的药代动力学特征。在大鼠中，AM-2099 表现出较低的总清除率和中等的 Vdss 和半衰期。相比之下，当在狗中给药时，AM-2099 显示出非常低的清除率、低 Vdss 和长半衰期 (18 小时)。与媒介物处理的动物相比，AM-2099 表明血浆暴露量呈剂量依赖性增加，同时抓挠次数呈剂量依赖性减少，在 60 mg/kg 剂量下观察到具有统计学意义的显著减少^[1]。

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

分子量

466.46

Formula

C₁₉H₁₃F₃N₄O₃S₂

CAS 号

1443373-17-8

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 : ≥ 150 mg/mL (321.57 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1438 mL	10.7190 mL	21.4381 mL
5 mM	0.4288 mL	2.1438 mL	4.2876 mL
10 mM	0.2144 mL	1.0719 mL	2.1438 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 (5.36 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.36 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

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: 98.06%

选择批次：

Data Sheet (645 KB) SDS (252 KB)

COA (292 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. [Content Brief]

Animal Administration ^[1]	Mice: AM-2099 (5, 20, 60 mg/kg) is dosed orally to C57BL/6 male mice 120 minutes prior to intradermal administration of histamine. Instances of scratching behavior are then measured over a 30-minute time period^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. [Content Brief]

AM-2099 相关分类

Neurological Disease

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	2.1438 mL	10.7190 mL	21.4381 mL	53.5952 mL
	5 mM	0.4288 mL	2.1438 mL	4.2876 mL	10.7190 mL
	10 mM	0.2144 mL	1.0719 mL	2.1438 mL	5.3595 mL
	15 mM	0.1429 mL	0.7146 mL	1.4292 mL	3.5730 mL
	20 mM	0.1072 mL	0.5360 mL	1.0719 mL	2.6798 mL
	25 mM	0.0858 mL	0.4288 mL	0.8575 mL	2.1438 mL
	30 mM	0.0715 mL	0.3573 mL	0.7146 mL	1.7865 mL
	40 mM	0.0536 mL	0.2680 mL	0.5360 mL	1.3399 mL
	50 mM	0.0429 mL	0.2144 mL	0.4288 mL	1.0719 mL
	60 mM	0.0357 mL	0.1787 mL	0.3573 mL	0.8933 mL
	80 mM	0.0268 mL	0.1340 mL	0.2680 mL	0.6699 mL
	100 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5360 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:

AM-20991443373-17-8AM2099AM 2099Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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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。

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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）

AM-2099

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