NR4A1 agonist 1
NR4A1 agonist 1 is a NR4A1 agonist with a Ki value of 2.96 μM. NR4A1 agonist 1 exhibits lipid-lowering activity in 3T3-L1 adipocytes, with an EC50 of 0.13 μM, significantly decreasing triglyceride (TG) accumulation and lipid droplet accumulation. NR4A1 agonist 1 can be used for the study of obesity.
For research use only. We do not sell to patients.
- CAS No.: 1825366-87-7
- Formula: C22H23N5O
- Molecular Weight:373.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All Nuclear Hormone Receptor 4A/NR4A Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 3T3-L1 | CC50 |
9.4 μM
Compound: 2; R17
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Cytotoxicity against confluent mouse 3T3-L1 preadipocytes assessed as reduction in cell viability measured after 24 hrs by SRB method
Cytotoxicity against confluent mouse 3T3-L1 preadipocytes assessed as reduction in cell viability measured after 24 hrs by SRB method
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[PMID: 38996004] |
| 3T3-L1 | EC50 |
0.086 μM
Compound: 2; R17
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Decrease in triglyceride level in mouse 3T3L1 preadipocytes compound treated for 6 days measured on day 6 by oil red O staining based microscopic analysis
Decrease in triglyceride level in mouse 3T3L1 preadipocytes compound treated for 6 days measured on day 6 by oil red O staining based microscopic analysis
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[PMID: 26572282] |
| 3T3-L1 | EC50 |
0.091 μM
Compound: R17
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Lipid lowering activity in mouse 3T3-L1 cells assessed as reduction in adipogenic cocktail-induced triglyceride levels incubated for 6 days by GPO-POD assay
Lipid lowering activity in mouse 3T3-L1 cells assessed as reduction in adipogenic cocktail-induced triglyceride levels incubated for 6 days by GPO-POD assay
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[PMID: 32163815] |
| 3T3-L1 | EC50 |
0.14 μM
Compound: 2; R17
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Lipid lowering activity in confluent mouse 3T3-L1 preadipocytes assessed as reduction in triglyceride level incubated for 9 days by oil red o staining based analysis
Lipid lowering activity in confluent mouse 3T3-L1 preadipocytes assessed as reduction in triglyceride level incubated for 9 days by oil red o staining based analysis
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[PMID: 38996004] |
| 3T3-L1 | IC50 |
34.4 μM
Compound: R17
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Cytotoxicity against mouse 3T3L1 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Cytotoxicity against mouse 3T3L1 cells assessed as decrease in cell viability after 24 hrs by MTT assay
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[PMID: 29425817] |
| HepG2 | IC50 |
27.4 μM
Compound: R17
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Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 24 hrs by MTT assay
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[PMID: 29425817] |
| RKO | IC50 |
1.7 μM
Compound: 2; R17
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Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs
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[PMID: 37253101] |
NR4A1 agonist 1 (Compound R17) (1-5 μM) concentration-dependently reduces F1 fluorescence intensity in si-NR4A1-transfected 3T3-L1 cells[1].
NR4A1 agonist 1 (0.125-0.25 μM) shows significantly attenuated TG-lowering effect compared to si-NC group in 3T3-L1 cells transfected with si-NR4A1[1].
NR4A1 agonist 1 (0.125-0.25 μM) decreases lipid droplet accumulation in si-NC-transfected 3T3-L1 cells[1].
NR4A1 agonist 1 (0.125-0.25 μM, 48 h) downregulates the mRNA expression levels of lipid anabolism-related genes FABP4, CD36, SLC25A10, SLC5A6, and ALDH2 in 3T3-L1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1825366-87-7
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Molecular Weight 373.45
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Formula C22H23N5O
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SMILES
CN(CCCNC1=NC(C2=C(C3=CC=CC=C3N2)C=O)=NC4=C1C=CC=C4)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NR4A1 agonist 1 Related Classifications
HY-175725 Related Classifications
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