Art. -Nr.: HY-130246

NF-56-EJ40

14 Cited Publications

Kundenbewertung

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 K_i of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a K_i value of 17.4 nM.

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Reinheit: 99.88%
CAS. Nr.: 2380230-73-7
Formel: C₂₇H₂₉N₃O₃
Molecular Weight:443.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

NF-56-EJ40 Chemical Structure

CAS. Nr.: 2380230-73-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

SUCNR1 (GPR91)^[1]

In Vitro

NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y83^2.64 and Y30^1.39 on one side, and R281^7.39 on the other side. The conserved E18^1.27 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E22^1.31 and N274^7.32 in human SUCNR1 are replaced by K181.31 and K269^7.32 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 Y30^1.39F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E18^1.27K and E18^1.27R 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 K18^1.31E/K269^7.32N (hereafter denoted humanized rat SUCNR1) (K_i 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.

Chemical Information

CAS. Nr. 2380230-73-7
Appearance Solid
Molecular Weight 443.54
Formel C₂₇H₂₉N₃O₃
Color Off-white to gray
SMILES

O=C(NC1=C(CC(O)=O)C=CC=C1)C2=CC=CC(C3=CC=C(CN4CCN(C)CC4)C=C3)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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J Clin Invest

Hyperglycemia aggravates vitiligo through succinate/SUCNR1-mediated T cell activation. [Abstract]

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).
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.
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.
Sci Adv

SUCNR1 coordinates metabolic flux, mitochondrial function, and nutrient-dependent adaptation in hepatocytes. [Abstract]

2026 Jun 12;12(24):eaec8873. PMID: 42284407
Metabolism

Protective effects of the succinate/SUCNR1 axis on damaged hepatocytes in NAFLD. [Abstract]

2023 Aug:145:155630. PMID: 37315889
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
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
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
Cell Signal

GPR91 mediates low shear stress-induced endothelial ferroptosis via EGR1-dependent GPX4 repression. [Abstract]

2025 Sep 10:136:112127. PMID: 40939914
bioRxiv

January 10, 2022.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2546 mL

11.2729 mL

22.5459 mL

5 mM

0.4509 mL

2.2546 mL

4.5092 mL

10 mM

0.2255 mL

1.1273 mL

2.2546 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Haffke M, et al. Structural basis of species-selective antagonist binding to the succinate receptor. Nature. 2019 Oct;574(7779):581-585. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

NF-56-EJ40

14 Cited Publications

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NF-56-EJ40

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) NF-56-EJ40

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NF-56-EJ40

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) NF-56-EJ40

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NF-56-EJ40 Related Classifications

HY-130246 Related Classifications