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

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

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PF-06471553

PF-06471553 構造式

CAS 番号 : 1808094-07-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 494 在庫あり
Solution
10 mM * 1 mL in DMSO USD 494 在庫あり
Solid
5 mg $480 在庫あり
10 mg $740 在庫あり
25 mg $1400 在庫あり
50 mg $2300 在庫あり
100 mg $3300 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

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]

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]
体外実験

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].

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

体内実験

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].

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

分子量

467.54

分子式

C23H25N5O4S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC2=C(CN(C(CC3=CC=CC(OC)=C3)=O)C2)C=C1)(NC4=NN(C5CCC5)N=C4)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 150 mg/mL (320.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2139 mL 1.0694 mL 2.1389 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます:C1V1 = C2V2

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純度とドキュメンテーション

純度: 98.29%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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  • Molarity Calculator

  • Dilution Calculator

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

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The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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Inquiry Information

製品名:
PF-06471553
製品番号:
HY-108339
数量:
MCE 日本正規代理店: