NF-56-EJ40
Based on 14 publication(s) in Google Scholar
NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.88%
- CAS 番号: 2380230-73-7
- 分子式: C27H29N3O3
- 分子量:443.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 NF-56-EJ40
More- Metabolism. 2023 Aug:145:155630. [Abstract]
- J Clin Invest. 2026 Jun 15;136(12):e200316. [Abstract]
- J Clin Invest. 2024 May 7:e173214. [Abstract]
- Sci Adv. 2026 Jun 12;12(24):eaec8873. [Abstract]
- Cardiovasc Res. 2024 Nov 25;120(14):1693-1712. [Abstract]
- Cancer Lett. 2022 Feb 1:526:91-102. [Abstract]
- Dev Cell. 2022 Sep 26;57(18):2221-2236.e5. [Abstract]
- Arch Pharm Res. 2025 Aug;48(7-8):782-797. [Abstract]
- J Agric Food Chem. 2024 Sep 25;72(38):21052-21064. [Abstract]
- Cell Signal. 2025 Sep 10:136:112127. [Abstract]
- Oncol Res. 2026 Jan 19;34(2):25. [Abstract]
- J Physiol. 2025 Mar 31. [Abstract]
- Poult Sci. 2024 Dec 31;104(2):104754. [Abstract]
- bioRxiv. January 10, 2022.
Customer Validation & Images
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RT-PCR
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ELISA
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WB
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IF
生物活性
SUCNR1 (GPR91)[1]
NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y832.64 and Y301.39 on one side, and R2817.39 on the other side. The conserved E181.27 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E221.31 and N2747.32 in human SUCNR1 are replaced by K181.31 and K2697.32 in rat SUCNR1. These two amino acid exchanges could prevent the binding of NF-56-EJ40 to rat SUCNR1 owing to steric hindrance. Radioligand-binding studies with human SUCNR1 showed partial agreement with our homology model: the Y301.39F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E181.27K and E181.27R mutants, probably owing to steric clashes of the Lys and Arg residues with NF-56-EJ40 and the loss of a hydrogen bond to its piperazine ring[1].
Human SUCNR1 residues are introduced into rat SUCNR1 to form the double mutant K181.31E/K2697.32N (hereafter denoted humanized rat SUCNR1) (Ki of 17.4 nM and 33.5 nM for human and humanized rat SUCNR1, respectively). NF-56-EJ40 increases the thermal stability of both humanized rat SUCNR1 and human SUCNR1, but not that of rat SUCNR1[1].
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 2380230-73-7
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性状 Solid
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分子量 443.54
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分子式 C27H29N3O3
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Color Off-white to gray
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SMILES
O=C(NC1=C(CC(O)=O)C=CC=C1)C2=CC=CC(C3=CC=C(CN4CCN(C)CC4)C=C3)=C2
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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 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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Metabolism
2023 Aug:145:155630. PMID: 37315889 -
J Clin Invest
2026 Jun 15;136(12):e200316. PMID: 42294897
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2026 Jun 15;136(12):e200316. [Abstract]
NF-56-EJ40 (50 nM; 3 h) markedly dampened succinate-induced increase of CXCL9 and CXCL10 mRNA in Normal human keratinocytes (NHKs).
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2026 Jun 15;136(12):e200316. [Abstract]
NF-56-EJ40 (50 nM; 3 h) markedly dampened succinate-induced increase of CXCL9 and CXCL10 protein in Normal human keratinocytes (NHKs).
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2026 Jun 15;136(12):e200316. [Abstract]
NF-56-EJ40 (50 nM; 3 h) reversed succinate-induced HIF-1α upregulation in Normal human keratinocytes (NHKs).
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2026 Jun 15;136(12):e200316. [Abstract]
NF-56-EJ40 (50 nM; 3 h) decreased HIF-1α expression in the cell nucleus in Normal human keratinocytes (NHKs).
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2026 Jun 15;136(12):e200316. [Abstract]
NF-56-EJ40 (50 nM; 3 h) inhibited the succinate-induced nuclear translocation of HIF-1α in Normal human keratinocytes (NHKs).
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J Clin Invest
SUCNR1 regulates insulin secretion and glucose elevates the succinate response in people with prediabetes. [Abstract]2024 May 7:e173214. PMID: 38713514
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 May 7:e173214. [Abstract]
NF-56-EJ40 (1 μM; 3 h) completely blocked succinate-induced insulin secretion in the presence of high glucose in EndoC-βH5 cells.
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Sci Adv
SUCNR1 coordinates metabolic flux, mitochondrial function, and nutrient-dependent adaptation in hepatocytes. [Abstract]2026 Jun 12;12(24):eaec8873. PMID: 42284407 -
Cardiovasc Res
miR-369-3p ameliorates diabetes-associated atherosclerosis by regulating macrophage succinate-GPR91 signaling. [Abstract]2024 Nov 25;120(14):1693-1712. PMID: 38703377
NF-56-EJ40 purchased from MedChemExpress. Usage Cited in: Cardiovasc Res. 2024 Nov 25;120(14):1693-1712. [Abstract]
NF-56-EJ40 (5 μM; 30 min+24 h) significantly reduced the OxLDL-induced IL-1β secretion in healthy and diabetic monocytes compared to control.
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Cancer Lett
Succinate receptor 1 inhibits mitochondrial respiration in cancer cells addicted to glutamine. [Abstract]2022 Feb 1:526:91-102. PMID: 34813893 -
Dev Cell
Pulmonary neuroendocrine cells sense succinate to stimulate myoepithelial cell contraction. [Abstract]2022 Sep 26;57(18):2221-2236.e5. PMID: 36108628 -
Arch Pharm Res
Silybin inhibits succinate production and secretion in hepatocytes to reverse liver fibrosis. [Abstract]2025 Aug;48(7-8):782-797. PMID: 40739373 -
J Agric Food Chem
Exposure to Succinate Leads to Steatosis in Non-Obese Non-Alcoholic Fatty Liver Disease by Inhibiting AMPK/PPARα/FGF21-Dependent Fatty Acid Oxidation. [Abstract]2024 Sep 25;72(38):21052-21064. PMID: 39268842 -
Cell Signal
GPR91 mediates low shear stress-induced endothelial ferroptosis via EGR1-dependent GPX4 repression. [Abstract]2025 Sep 10:136:112127. PMID: 40939914 -
Oncol Res
SDHA Deficiency in Hepatocellular Carcinoma Promotes Tumor Progression through Succinate-Induced M2 Macrophage Polarization. [Abstract]2026 Jan 19;34(2):25. PMID: 41613800 -
J Physiol
Impaired angiogenesis in gestational diabetes is linked to succinate/SUCNR1 axis dysregulation in late gestation. [Abstract]2025 Mar 31. PMID: 40163642 -
Poult Sci
Lactobacillus salivarius metabolite succinate enhances chicken intestinal stem cell activities via the SUCNR1-mitochondria axis. [Abstract]2024 Dec 31;104(2):104754. PMID: 39764876 -
溶剤 & 溶解度
DMSO : 5 mg/mL (11.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4.55 mg/mL (10.26 mM; ultrasonic and adjust pH to 9 with NaOH)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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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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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2546 mL | 11.2729 mL | 22.5459 mL | 56.3647 mL |
| 5 mM | 0.4509 mL | 2.2546 mL | 4.5092 mL | 11.2729 mL | |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2546 mL | 5.6365 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
NF-56-EJ40 関連分類
HY-130246 関連分類
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