Nurr1/RXR agonist 1

Name: Nurr1/RXR agonist 1
Brand: MedChemExpress
SKU: HY-180576
Rating: 4.5 (0 reviews)

Cat. No.: HY-180576 Purity: 98.26%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC₅₀ = 2.6 µM) and RXR with Ks of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research.

For research use only. We do not sell to patients.

Nurr1/RXR agonist 1 Chemical Structure

CAS No. : 2231746-53-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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RXRα RXRβ RXRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC₅₀ = 2.6 µM) and RXR with K^[1]s of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research^[1].

IC₅₀ & Target^[1]

Nurr1/NR4A2

In Vitro

Nurr1/RXR agonist 1 (compound 2) (15 h) induces a considerable 3.3-fold activation of Nurr1, with both Nurr1 and RXR involved^[1].
Nurr1/RXR dual agonist 1 (30 μM) diminishes Nurr1 homodimer formation while leaving the Nurr1:RXR heterodimer intact^[1].
Nurr1/RXR agonist 1 (0.3-30 μM) enhances DR5-dependent transcription but does not activate NBRE or NurRE^[1].
Nurr1/RXR agonist 1 (0.3-30 μM, 24 h) exhibits no toxic effect in HEK293T cells^[1].
Nurr1/RXR agonist 1 (10 μM, 21 h) achieves differential modulation or functional selectivity in activating downstream gene expression programs in rat dopaminergic neurons^[1].
Nurr1/RXR agonist 1 induces genes that have a higher empirical probability of containing DR5 elements in their promoter regions^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[1]

Cell Line:	rat dopaminergic neurons
Concentration:	10 μM
Incubation Time:	21 h
Result:	Induced the expression of tyrosine hydroxylase (TH), fibronectin leucine rich transmembrane protein 2 (FLRT2), brain-derived neurotrophic factor (BDNF) and collapsin response mediator protein 4 (CRMP4; Dpysl3 in rat). Did not induced X-linked inhibitor of apoptosis protein (XIAP), sestrin 3 (SESN3), cyclin D2 (CCND2), baculoviral inhibitor of apoptosis repeat-containing 5 (BIRC5), and superoxide dismutase 2 (SOD2).

Molecular Weight

319.35

Formula

C₁₈H₁₉F₂NO₂

CAS No.

2231746-53-3

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=CC=C(N2C(C)=C(C)C3=C2CCC(F)(F)C3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (313.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1314 mL	15.6568 mL	31.3136 mL
5 mM	0.6263 mL	3.1314 mL	6.2627 mL
10 mM	0.3131 mL	1.5657 mL	3.1314 mL

View the 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.26%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (254 KB) HNMR (263 KB) RP-HPLC (243 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Scholz K, et al. Dual Nurr1/RXR agonism of valerenic acid and synthetic mimetics enables dimer-selective Nurr1 modulation. ACS Med Chem Lett. 2026 Jan 8;17(1):170-174. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1314 mL	15.6568 mL	31.3136 mL	78.2840 mL
	5 mM	0.6263 mL	3.1314 mL	6.2627 mL	15.6568 mL
	10 mM	0.3131 mL	1.5657 mL	3.1314 mL	7.8284 mL
	15 mM	0.2088 mL	1.0438 mL	2.0876 mL	5.2189 mL
	20 mM	0.1566 mL	0.7828 mL	1.5657 mL	3.9142 mL
	25 mM	0.1253 mL	0.6263 mL	1.2525 mL	3.1314 mL
	30 mM	0.1044 mL	0.5219 mL	1.0438 mL	2.6095 mL
	40 mM	0.0783 mL	0.3914 mL	0.7828 mL	1.9571 mL
	50 mM	0.0626 mL	0.3131 mL	0.6263 mL	1.5657 mL
	60 mM	0.0522 mL	0.2609 mL	0.5219 mL	1.3047 mL
	80 mM	0.0391 mL	0.1957 mL	0.3914 mL	0.9786 mL
	100 mM	0.0313 mL	0.1566 mL	0.3131 mL	0.7828 mL