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

PF-06471553 是一種有效的,選擇性的,可口服的 monoacylglycerol acyltransferase 3 (MGAT3) 抑制劑,IC50 值為 92 nM。

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PF-06471553 Chemical Structure

PF-06471553 Chemical Structure

CAS No. : 1808094-07-6

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規(guī)格 價(jià)格 是否有貨 數(shù)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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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 Acyltransferase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]

細(xì)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]
體外研究
(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.

體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 150 mg/mL (320.83 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.29%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 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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產(chǎn)品名稱:
PF-06471553
目錄號(hào):
HY-108339
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