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Nrf2 activator-3

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Nrf2 activator-3 is a potent Nrf2 activator. Nrf2 activator-3 is used for cerebral ischemic injury research.

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Pureté: 99.50%
CAS No.: 2766570-23-2
Formule: C₂₃H₁₈F₃N₃O₂
Masse moléculaire:425.40

Stockage:

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

Nrf2 activator-3 Chemical Structure

CAS No.: 2766570-23-2

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Nrf2 activator-3 is a potent Nrf2 activator. Nrf2 activator-3 is used for cerebral ischemic injury research^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
HaCaT	IC₅₀	126.7 μM Compound: 24	Cytotoxicity against human HaCaT cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HaCaT cells assessed as reduction in cell viability by MTT assay	[PMID: 35390713]
PC-12	IC₅₀	262.7 μM Compound: 24	Cytotoxicity against rat PC-12 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against rat PC-12 cells assessed as reduction in cell viability by MTT assay	[PMID: 35390713]

In Vitro

Nrf2 activator-3 (compound 24) (1 μM, 5 μM, and 10 μM) is against SNP (400 μM)-induced cell death with IC₅₀ values of 76.86±3.54 μM, 101.59±3.34 μM, and 105.1±1.84 μM at 1 μM, 5 μM, and 10 μM, respectively in PC12 cells^[1].
Nrf2 activator-3 (1-200 μM) is against PC12 and hacat cell with IC₅₀ values of 262.70±1.98 μM and 126.70±10.39 μM, respctively^[1].

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

Cell Viability Assay^[1]

Cell Line:

PC12 cell
Concentration:

1 μM, 5 μM, and 10 μM
Incubation Time:
Result:

Alleviated SNP-induced apoptosis in a concentration-dependent manner.

In Vivo

In the acute toxicity study, Nrf2 activator-3 (compound 24) shows toxicity to the experimental mice at 1000 mg/kg, the LD50 of intraperitoneal injection is 789 mg/kg, and the 95% confidence interval was 550-1000 mg/kg in balb/c mice^[1].
In in vivo pharmacokinetic properties study, Nrf2 activator-3 (5 mg/kg; Intraperitoneal injection) shows that plasma reached a maximum (323.06 ng/mL) at 2 h. The T_max, C_max, AUC_0-inf, F% and T_1/2 values are 2 hour, 323.06 ng/mL, 2929.88 ng/mL*h, 28%, 12.75 hours respctively^[1].
Nrf2 activator-3 (5 mg/kg; .i.v.) shows T_max, C_max, AUC_0-inf, and T_1/2 values are 0.08 hours, 6911.14 ng/mL, 10182.73 ng/mL*h, and 8.26 hours respctively^[1].
Nrf2 activator-3 (3 mg/kg; 10 mg/kg;30 mg/kg) reduces the cerebral infarction volume and leads to decreased neurological deficits in MCAO rats^[1].

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

Animal Model:

MCAO rats
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

Intraperitoneal injection
Result:

Attenuated cerebral ischemic injury.
(low dose: 16.37 ± 6.51%, medium dose: 14.49 ± 5.62%, high dose: 12.23 ± 8.50%), which was similar to the effect of Edaravone (12.77 ± 5.82%).

Animal Model:

MCAO rats
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

Intraperitoneal injection
Result:

Attenuated cerebral ischemic injury.
(low dose: 16.37 ± 6.51%, medium dose: 14.49 ± 5.62%, high dose: 12.23 ± 8.50%), which was similar to the effect of Edaravone (12.77 ± 5.82%).

Chemical Information

CAS No. 2766570-23-2
Appearance Solid
Masse moléculaire 425.40
Formule C₂₃H₁₈F₃N₃O₂
Color Off-white to light yellow
SMILES

CC1=CC(C)=CC(N2N=C(N=C2C3=C(C=CC=C3)O)C4=CC=C(C=C4O)C(F)(F)F)=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Free Radic Biol Med

APOE4 impairs Nrf2-PINK1/Parkin-dependent mitochondrial clearance through disrupted antioxidant and mitophagy signaling. [Abstract]

2025 Nov 21:243:245-259. PMID: 41275935

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (235.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.3507 mL

11.7536 mL

23.5073 mL

5 mM

0.4701 mL

2.3507 mL

4.7015 mL

10 mM

0.2351 mL

1.1754 mL

2.3507 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.88 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (251 KB)
- English - EN (251 KB)
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- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Yaoqiang Lao, et al. Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury. Eur J Med Chem. 2022 Jun 5;236:114315. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3507 mL	11.7536 mL	23.5073 mL	58.7682 mL
	5 mM	0.4701 mL	2.3507 mL	4.7015 mL	11.7536 mL
	10 mM	0.2351 mL	1.1754 mL	2.3507 mL	5.8768 mL
	15 mM	0.1567 mL	0.7836 mL	1.5672 mL	3.9179 mL
	20 mM	0.1175 mL	0.5877 mL	1.1754 mL	2.9384 mL
	25 mM	0.0940 mL	0.4701 mL	0.9403 mL	2.3507 mL
	30 mM	0.0784 mL	0.3918 mL	0.7836 mL	1.9589 mL
	40 mM	0.0588 mL	0.2938 mL	0.5877 mL	1.4692 mL
	50 mM	0.0470 mL	0.2351 mL	0.4701 mL	1.1754 mL
	60 mM	0.0392 mL	0.1959 mL	0.3918 mL	0.9795 mL
	80 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7346 mL
	100 mM	0.0235 mL	0.1175 mL	0.2351 mL	0.5877 mL

Keywords

Nrf2 activator-3

1 Cited Publications

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Nrf2 activator-3

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Publications Citing Use of MedChemExpress (MCE) Nrf2 activator-3

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Nrf2 activator-3

Immunology/Inflammation Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Pulmonary Fibrosis Compound Library

Radioprotector 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) Nrf2 activator-3

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Nrf2 activator-3 Related Classifications

HY-143333 Related Classifications