1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. PF-06471553

PF-06471553 是一种有效的,选择性的,可口服的 monoacylglycerol acyltransferase 3 (MGAT3) 抑制剂,IC50 值为 92 nM。

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PF-06471553 Chemical Structure

PF-06471553 Chemical Structure

CAS No. : 1808094-07-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5280
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1 mg ¥2181
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5 mg ¥4800
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Acyltransferase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

IC50 & Target

IC50: 92 nM (MGAT3)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
205 nM
Compound: 6f
Inhibition of human MGAT3 expressed in HEK293 cells assessed as effect on incorporation of [1,3-14C] glycerol into TAG by TLC method in presence of DGAT1 inhibitor PF-04620110 and DGAT2 inhibitor PF-06424439
Inhibition of human MGAT3 expressed in HEK293 cells assessed as effect on incorporation of [1,3-14C] glycerol into TAG by TLC method in presence of DGAT1 inhibitor PF-04620110 and DGAT2 inhibitor PF-06424439
[PMID: 26258602]
体外研究
(In Vitro)

PF-06471553 (6f) is a potent and selective monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM, and shows >160 fold in vitro selectivity for MGAT3 over DGAT1 (IC50, >50 μM), DGAT2 (IC50, >100 μM), MGAT1 (IC50, 14.9 μM), and MGAT2 (IC50, 19.8 μM). PF-06471553 exhibits inhibitory activity against MGAT3 in HEK-293 cells with an IC50 of 205 nM (pIC50, 6.69)[1].

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

体内研究
(In Vivo)

PF-06471553 (200 mg/kg, p.o.) in addition with (DGAT1 and DGAT2) inhibitors shows additional inhibition of glycerol-d5 incorporated triolein in hMGAT3 mice, and with no effect on WT mice[1].

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

分子量

467.54

Formula

C23H25N5O4S

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

DMSO 中的溶解度 : ≥ 150 mg/mL (320.83 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 2.1389 mL 10.6943 mL 21.3885 mL
5 mM 0.4278 mL 2.1389 mL 4.2777 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

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

纯度: 98.29%

参考文献

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 2.1389 mL 10.6943 mL 21.3885 mL 53.4714 mL
5 mM 0.4278 mL 2.1389 mL 4.2777 mL 10.6943 mL
10 mM 0.2139 mL 1.0694 mL 2.1389 mL 5.3471 mL
15 mM 0.1426 mL 0.7130 mL 1.4259 mL 3.5648 mL
20 mM 0.1069 mL 0.5347 mL 1.0694 mL 2.6736 mL
25 mM 0.0856 mL 0.4278 mL 0.8555 mL 2.1389 mL
30 mM 0.0713 mL 0.3565 mL 0.7130 mL 1.7824 mL
40 mM 0.0535 mL 0.2674 mL 0.5347 mL 1.3368 mL
50 mM 0.0428 mL 0.2139 mL 0.4278 mL 1.0694 mL
60 mM 0.0356 mL 0.1782 mL 0.3565 mL 0.8912 mL
80 mM 0.0267 mL 0.1337 mL 0.2674 mL 0.6684 mL
100 mM 0.0214 mL 0.1069 mL 0.2139 mL 0.5347 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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产品名称:
PF-06471553
目录号:
HY-108339
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