Nrf2 activator-4

Name: Nrf2 activator-4
Brand: MedChemExpress
SKU: HY-146086
Rating: 4.5 (1 reviews)

Cat. No.: HY-146086 Purity: 98.53%: FAQs
Data Sheet SDS COA Handling Instructions

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Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC₅₀ of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model.

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

Nrf2 activator-4 Chemical Structure

CAS No. : 2383016-68-8

Size	Price	Stock	Quantity
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

EC₅₀: 0.63 µM (Nrf2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
U2OS	EC₅₀	0.63 μM Compound: 20a	Activation of NRF2 in human U2OS cells co-expressing Keap1 (unknown origin) assessed as induction of NRF2 translocation to nucleus incubated for 6 hrs by beta-galactosidase based chemiluminescent assay Activation of NRF2 in human U2OS cells co-expressing Keap1 (unknown origin) assessed as induction of NRF2 translocation to nucleus incubated for 6 hrs by beta-galactosidase based chemiluminescent assay	[PMID: 31670201]

Molecular Weight

468.90

Formula

C₂₃H₂₄ClF₃N₂O₃

CAS No.

2383016-68-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(C=C1)OCC(N2CCN(CC2)C)=O)/C=C/C3=C(C=CC=C3)C(F)(F)F.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (213.27 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	2.1327 mL	10.6633 mL	21.3265 mL
5 mM	0.4265 mL	2.1327 mL	4.2653 mL
10 mM	0.2133 mL	1.0663 mL	2.1327 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (5.33 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 (5.33 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 (5.33 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 and light)

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: 98.53%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (245 KB) HNMR (277 KB) RP-HPLC (258 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Kim HJ, et al. A novel chalcone derivative as Nrf2 activator attenuates learning and memory impairment in a scopolamine-induced mouse model. Eur J Med Chem. 2020 Jan 1;185:111777. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1327 mL	10.6633 mL	21.3265 mL	53.3163 mL
	5 mM	0.4265 mL	2.1327 mL	4.2653 mL	10.6633 mL
	10 mM	0.2133 mL	1.0663 mL	2.1327 mL	5.3316 mL
	15 mM	0.1422 mL	0.7109 mL	1.4218 mL	3.5544 mL
	20 mM	0.1066 mL	0.5332 mL	1.0663 mL	2.6658 mL
	25 mM	0.0853 mL	0.4265 mL	0.8531 mL	2.1327 mL
	30 mM	0.0711 mL	0.3554 mL	0.7109 mL	1.7772 mL
	40 mM	0.0533 mL	0.2666 mL	0.5332 mL	1.3329 mL
	50 mM	0.0427 mL	0.2133 mL	0.4265 mL	1.0663 mL
	60 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8886 mL
	80 mM	0.0267 mL	0.1333 mL	0.2666 mL	0.6665 mL
	100 mM	0.0213 mL	0.1066 mL	0.2133 mL	0.5332 mL

Nrf2 activator-4 Related Classifications

Neurological Disease Inflammation/Immunology

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:

Nrf2 activator-42383016-68-8Keap1-Nrf2Reactive Oxygen SpeciesAlzheimer’s diseaseanti-inflammatorysuperoxide dismutaseBV-2antioxidantInhibitorinhibitorinhibit

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Nrf2 activator-4

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Complete Stock Solution Preparation Table

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