2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF-06649298

PF-06649298 是一个 sodium-coupled citrate transporter (NaCT or SLC13A5) 抑制剂。PF-06649298 在人类肝细胞中与 NaCT 结合从而抑制柠檬酸盐运输，其 IC50 值为 16.2 μM。PF-06649298 可用于调节糖代谢以及脂代谢的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PF-06649298 Chemical Structure

PF-06649298 Chemical Structure

CAS No. : 1854061-16-7

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4950
In-stock
1 mg ￥2045
In-stock
5 mg ￥4500
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

PF-06649298 相关抗体

Top Publications Citing Use of Products

查看 Sodium Channel 亚型特异性产品:

查看所有亚型
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism[1][2].

IC50 & Target

IC50: 408 nM (citrate uptake in HEKNaCT), 16.2 μM (citrate uptake in Human Heps), 4.5 μM (citrate uptake in Mouse Heps), ＞100 μM (citrate uptake in HEKNaCD1), ＞100 μM (citrate uptake in HEKNaCD3)[1][2]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 100 μM
Compound: 1a; PF-06649298
Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
[PMID: 26734723]
HEK293 IC50
> 100 μM
Compound: 1a; PF-06649298
Inhibition of NaDC3 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
Inhibition of NaDC3 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
[PMID: 26734723]
HEK293 IC50
0.41 μM
Compound: 1a; PF-06649298
Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
[PMID: 26734723]
Hepatocyte IC50
16.2 μM
Compound: 1a; PF-06649298
Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
[PMID: 26734723]
体外研究
(In Vitro)

PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[1].

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

PF-06649298 相关抗体:

Cell Viability Assay[1]

Cell Line: HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes
Concentration: 0-100 μM
Incubation Time: 30 min
Result: Showed a selectivity for NaCT over the dicarboxylate transporters NaDC1 and NaDC3. Inhibited citrate uptake in HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes with IC50s of 408 nM, ＞100 μM, ＞100 μM, 16.2 μM and 4.5 μM, respectively.
体内研究
(In Vivo)

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice[2].

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

Animal Model: Mice with high fat diet (HFD) administration[2]
Dosage: 250 mg/kg
Administration: Oral gavage; 250mg/kg twice a day; for 21 days
Result: Decreased plasma glucose, hepatic triglycerides, diacylglycerides, and acyl-carnitines concentration of livers in HFD mice. Totally reversed glucose intolerance of HFD mice.
分子量

294.34

Formula

C16H22O5
CAS 号
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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (339.74 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 3.3974 mL 16.9872 mL 33.9743 mL
5 mM 0.6795 mL 3.3974 mL 6.7949 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PF-06649298 相关分类

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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3974 mL 16.9872 mL 33.9743 mL 84.9358 mL
5 mM 0.6795 mL 3.3974 mL 6.7949 mL 16.9872 mL
10 mM 0.3397 mL 1.6987 mL 3.3974 mL 8.4936 mL
15 mM 0.2265 mL 1.1325 mL 2.2650 mL 5.6624 mL
20 mM 0.1699 mL 0.8494 mL 1.6987 mL 4.2468 mL
25 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3974 mL
30 mM 0.1132 mL 0.5662 mL 1.1325 mL 2.8312 mL
40 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1234 mL
50 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
60 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4156 mL
80 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
100 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8494 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-066492981854061-16-7PF06649298PF 06649298Sodium ChannelNa channelsNa+ channelscitrateglucose intoleranceHFDDIOdiacylglyceridehepatic triglycerideacyl-carnitineInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PF-06649298
目录号：
HY-120103
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z