PF-06471553
Based on 1 publication(s) in Google Scholar
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.07%
- CAS 番号: 1808094-07-6
- 分子式: C23H25N5O4S
- 分子量:467.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 PF-06471553
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生物活性
IC50: 92 nM (MGAT3)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
205 nM
Compound: 6f
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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
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[PMID: 26258602] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1808094-07-6
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性状 Solid
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分子量 467.54
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分子式 C23H25N5O4S
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Color White to off-white
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SMILES
O=S(C1=CC2=C(CN(C(CC3=CC=CC(OC)=C3)=O)C2)C=C1)(NC4=NN(C5CCC5)N=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Clin Invest
MOGAT3-Mediated DAG Accumulation Drives Acquired Resistance to Anti-BRAF/EGFR Therapy in BRAFV600E-Mutant Metastatic Colorectal Cancer. [Abstract]2024 Oct 22;134(24):e182217. PMID: 39436710
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
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 |