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  2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF-01247324

PF-01247324是選擇性且有口服活性的Nav1.8通道阻斷物，對人類重組Nav1.8 的IC50值為196 nM。

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PF-01247324 Chemical Structure

PF-01247324 Chemical Structure

CAS No. : 875051-72-2

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規(guī)格 價格 是否有貨 數(shù)量
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
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100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 Sodium Channel 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.

IC50 & Target

IC50: 196 nM (hNav1.8)[1]
細(xì)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]
體外研究
(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 Nav1.8 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.
體內(nèi)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 號
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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 : ≥ 30 mg/mL (90.74 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

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

動物實(shí)驗(yàn)：

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

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 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

    請依序添加每種溶劑： 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 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲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: 99.63%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?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 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
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    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：
PF-01247324
目錄號：
HY-101383
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