NR4A1 agonist 1

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NR4A1 agonist 1 is a NR4A1 agonist with a K_i 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.

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NR4A1 agonist 1 Chemical Structure

CAS No. : 1825366-87-7

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
3T3-L1	CC₅₀	9.4 μM Compound: 2; R17	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	[PMID: 38996004]
3T3-L1	EC₅₀	0.086 μM Compound: 2; R17	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	[PMID: 26572282]
3T3-L1	EC₅₀	0.091 μM Compound: R17	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	[PMID: 32163815]
3T3-L1	EC₅₀	0.14 μM Compound: 2; R17	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	[PMID: 38996004]
3T3-L1	IC₅₀	34.4 μM Compound: R17	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	[PMID: 29425817]
HepG2	IC₅₀	27.4 μM Compound: R17	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	[PMID: 29425817]
RKO	IC₅₀	1.7 μM Compound: 2; R17	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	[PMID: 37253101]

In Vitro

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.

Molecular Weight

373.45

Formula

C₂₂H₂₃N₅O

CAS No.

1825366-87-7

SMILES

CN(CCCNC1=NC(C2=C(C3=CC=CC=C3N2)C=O)=NC4=C1C=CC=C4)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hu YT, et al. Identification of Indoquinazoline Derivatives as Novel NR4A1 Agonists by Suppressing Adipocyte Lipogenesis for Treatment of Obesity. J Med Chem. 2025 Aug 28;68(16):17364-17377. [Content Brief]

NR4A1 agonist 1 Related Classifications

Metabolic Disease

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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.

Keywords:

NR4A1 agonist 11825366-87-7Nuclear Hormone Receptor 4A/NR4ANuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorobesityNR4A13T3-L1triglyceridelipid dropletInhibitorinhibitorinhibit

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