2. NF-κB
  3. Keap1-Nrf2
  4. Nrf2 activator-3

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

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Nrf2 activator-3 Chemical Structure

Nrf2 activator-3 Chemical Structure

CAS No. : 2766570-23-2

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Based on 1 publication(s) in Google Scholar

Nrf2 activator-3 Related Antibodies

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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.

Nrf2 activator-3 Related Antibodies

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 Tmax, Cmax, AUC0-inf, F% and T1/2 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 Tmax, Cmax, AUC0-inf, and T1/2 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%).
Molecular Weight

425.40

Formula

C23H18F3N3O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3507 mL 11.7536 mL 23.5073 mL
5 mM 0.4701 mL 2.3507 mL 4.7015 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. 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    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

mg/kg

Animal weight
(per animal)

g

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).
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
References

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. 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
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Nrf2 activator-3 Related Classifications

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-32766570-23-2Keap1-Nrf2Nrf2cerebralischemicinjurystrokecerebral diseaseInhibitorinhibitorinhibit

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