Nrf2 activator-6

Cat. No.: HY-148480: FAQs
Data Sheet Handling Instructions

Molarity Calculator

Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC₅₀ of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4).

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

Nrf2 activator-6 Chemical Structure

CAS No. : 2728780-74-1

Size	Price	Stock
1 mg	USD 670	Ask For Quote & Lead Time
5 mg	USD 2000	Ask For Quote & Lead Time
10 mg	USD 3400	Ask For Quote & Lead Time
25 mg	USD 6860	Ask For Quote & Lead Time
50 mg	USD 11660	Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

Nrf2 activator-6 (Example 4) increases the mRNA level of NRF2 mediated gene NADPH:quinone acceptor oxidoreductase 1 (NQO1), with an EC₅₀ of 0.3 nM^[1].

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

Molecular Weight

614.11

Formula

C₃₁H₃₇ClFN₅O₅

CAS No.

2728780-74-1

Appearance

Solid

Color

White to off-white

SMILES

OC([C@@](C)(CCC1)[C@@H]1C(N2[C@H](CN3C(CC4(C3)CC4)=O)C5=C(C(F)=CC(Cl)=C5CC2)OCC6=C7N(CCCC7)N=N6)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (162.84 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	1.6284 mL	8.1419 mL	16.2837 mL
5 mM	0.3257 mL	1.6284 mL	3.2567 mL
10 mM	0.1628 mL	0.8142 mL	1.6284 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)

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 (4.07 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 (4.07 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 (4.07 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).

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

Handling Instructions (2659 KB)

References

[1]. Cathy Louise LUCAS, et al. Tetrahydroisoquinoline compounds as nrf2 activators. WO2021214470A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6284 mL	8.1419 mL	16.2837 mL	40.7093 mL
	5 mM	0.3257 mL	1.6284 mL	3.2567 mL	8.1419 mL
	10 mM	0.1628 mL	0.8142 mL	1.6284 mL	4.0709 mL
	15 mM	0.1086 mL	0.5428 mL	1.0856 mL	2.7140 mL
	20 mM	0.0814 mL	0.4071 mL	0.8142 mL	2.0355 mL
	25 mM	0.0651 mL	0.3257 mL	0.6513 mL	1.6284 mL
	30 mM	0.0543 mL	0.2714 mL	0.5428 mL	1.3570 mL
	40 mM	0.0407 mL	0.2035 mL	0.4071 mL	1.0177 mL
	50 mM	0.0326 mL	0.1628 mL	0.3257 mL	0.8142 mL
	60 mM	0.0271 mL	0.1357 mL	0.2714 mL	0.6785 mL
	80 mM	0.0204 mL	0.1018 mL	0.2035 mL	0.5089 mL
	100 mM	0.0163 mL	0.0814 mL	0.1628 mL	0.4071 mL

Nrf2 activator-6 Related Classifications

Cardiovascular Disease

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-62728780-74-1Keap1-Nrf2Nrf2 activatortetrahydroisoquinolineKelch domain-Nrf2 interactionNQO1Inhibitorinhibitorinhibit

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