PF-01247324

目录号: HY-101383 纯度: 99.63%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

PF-01247324是选择性且有口服活性的Na_v1.8通道阻断物，对人类重组Na_v1.8 的IC₅₀值为196 nM。

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PF-01247324 Chemical Structure

CAS No. : 875051-72-2

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3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
5 mg	￥700	In-stock
10 mg	￥1200	In-stock
25 mg	￥2600	In-stock
50 mg	￥4500	In-stock
100 mg	现货	询价
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 1 篇科研文献

•Front Pharmacol. 16 December 2021.

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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

PF-01247324 is a selective and orally bioavailable Na_v1.8 channel blocker with an IC₅₀ of 196 nM for recombinant human Na_v1.8 channel.

IC₅₀ & Target

IC50: 196 nM (hNa_v1.8)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.19 μM Compound: 3	Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology	[PMID: 26101568]
HEK293	IC₅₀	12.8 μM Compound: 3	Inhibition of human Nav1.2 expressed in HEK293 cells by IonWorks Quattro selectivity assay Inhibition of human Nav1.2 expressed in HEK293 cells by IonWorks Quattro selectivity assay	[PMID: 26101568]
HEK293	IC₅₀	13 μM Compound: 3	Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay	[PMID: 26101568]
HEK293	IC₅₀	19 μM Compound: 3	Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay	[PMID: 26101568]
HEK293	IC₅₀	2.6 μM Compound: 3	Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]
HEK293	IC₅₀	9 μM Compound: 3	Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay	[PMID: 26101568]
SH-SY5Y	IC₅₀	14 μM Compound: 3	Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]
SH-SY5Y	IC₅₀	14 μM Compound: 3	Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]
SH-SY5Y	IC₅₀	14 μM Compound: 3	Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]

体外研究
(In Vitro)

PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC₅₀=331 nM) and in recombinantly expressed h Na_v1.8 channels (IC₅₀=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC₅₀=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC₅₀=10-18 μM). In vitro current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential^[1].

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

体内研究
(In Vivo)

Experiments n rodents demonstrates efficacy in both inflammatory and neuropathic pain models. PF-01247324 reduces phase 2 flinching by 37% at 100 mg/kg. There is a significant effect of 30 mg/kg of PF-01247324 in the rat model carrageenan-induced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126 μM respectively^[1]. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control^[2].

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

分子量

330.60

Formula

C₁₃H₁₀Cl₃N₃O

CAS 号

875051-72-2

性状

固体

颜色

Off-white to light yellow

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 : ≥ 30 mg/mL (90.74 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	3.0248 mL	15.1240 mL	30.2480 mL
5 mM	0.6050 mL	3.0248 mL	6.0496 mL
10 mM	0.3025 mL	1.5124 mL	3.0248 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 (7.56 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 (7.56 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.56 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: 99.63%

选择批次：

Data Sheet (626 KB) SDS (420 KB)

COA (286 KB) LCMS (98 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. [Content Brief]

[2]. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. [Content Brief]

Animal Administration ^[1]^[2]	Rats: For male Sprague Dawley rats (170-300 g), PF-01247324 is formulated as solutions of 0, 10, 30, 100 mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioural testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted^[1]. Mice: PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of vehicle^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. [Content Brief] [2]. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. [Content Brief]

Animal Administration
^[1]^[2]

Rats: For male Sprague Dawley rats (170-300 g), PF-01247324 is formulated as solutions of 0, 10, 30, 100 mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioural testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted^[1].

Mice: PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of vehicle^[2].

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

参考文献

[1]. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. [Content Brief]

[2]. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. [Content Brief]

PF-01247324 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	3.0248 mL	15.1240 mL	30.2480 mL	75.6201 mL
	5 mM	0.6050 mL	3.0248 mL	6.0496 mL	15.1240 mL
	10 mM	0.3025 mL	1.5124 mL	3.0248 mL	7.5620 mL
	15 mM	0.2017 mL	1.0083 mL	2.0165 mL	5.0413 mL
	20 mM	0.1512 mL	0.7562 mL	1.5124 mL	3.7810 mL
	25 mM	0.1210 mL	0.6050 mL	1.2099 mL	3.0248 mL
	30 mM	0.1008 mL	0.5041 mL	1.0083 mL	2.5207 mL
	40 mM	0.0756 mL	0.3781 mL	0.7562 mL	1.8905 mL
	50 mM	0.0605 mL	0.3025 mL	0.6050 mL	1.5124 mL
	60 mM	0.0504 mL	0.2521 mL	0.5041 mL	1.2603 mL
	80 mM	0.0378 mL	0.1891 mL	0.3781 mL	0.9453 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:

PF-01247324875051-72-2PF01247324PF 01247324Sodium 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。

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）

PF-01247324

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献