2. NF-κB
  3. Keap1-Nrf2
  4. NXPZ-2

NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research.

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NXPZ-2 Chemical Structure

NXPZ-2 Chemical Structure

CAS No. : 2254492-08-3

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Based on 1 publication(s) in Google Scholar

NXPZ-2 Related Antibodies

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Description

NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research[1].

IC50 & Target

Ki: 95 nM (Keap 1); EC50: 120 and 170 nM (Keap 1) [1]
In Vitro

NXPZ-2 (0-200 μM, 7 days) has no obvious toxicity on primary cortical neuron[1].

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

NXPZ-2 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: primary cortical neuron
Concentration: 0, 1.6, 8, 40 and 200 μM
Incubation Time: 7 days
Result: Had no obvious toxicity on primary cortical neuron [1].
In Vivo

NXPZ-2 (Male ICR mice, 52.5/105/210 mg/kg, p.o., once daily for 7 days) improves AD mice learning and memorizing function including increased spontaneous alternation, increases number of active avoidance times, shortened escape latency, increased the time spent in the target quadrant and number of platform crossing[1].
NXPZ-2 (Male ICR mice, 52.5/105/210 mg/kg, p.o., once daily for 7 days) rescues the brain structure damage and lowers dead neuron numbers of AD mice with no obvious toxicity on mouse organs[1].
NXPZ-2 (Male ICR mice, 52.5/105/210 mg/kg, p.o., once daily for 7 days) alleviates oxidative stress by increasing Nrf2 expression levels, and promotes Nrf2’s cytoplasm to nuclear translocation, and improves cognitive dysfunction by elevating Nrf2 in both the central nervous system and peripheral blood[1].

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

Animal Model: Male ICR mice, AD model[1].
Dosage: 52.5 mg/kg, 105 mg/kg, 210 mg/kg.
Administration: P.o., once daily for 7 days.
Result: Showed statistically increased spontaneous alternation and no influence on basal motivation, displayed an increased number of active avoidance times, which improved the learning and memory ability of AD mice. Cell number and morphology in NPZX-2-treated groups were restored, dead neuron numbers of AD mice was lowered.
Increased serum Nrf2 level, displays more Nrf2 in the hippocampal and cortical nucleus and less expression level in the hippocampal and cortical cytoplasm. Increased Nrf2-ARE binding in both hippocampus and frontal cortex, dose-dependently restored SOD, GSH, and MDA levels, and decreased AD marker protein (p-Tau)[1].
Molecular Weight

597.66

Formula

C27H27N5O7S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)CN(C1=C2C=CC=CC2=C(N(CC(N)=O)S(=O)(C3=CC=C(N)C=C3)=O)C=C1)S(=O)(C4=CC=C(OC)C=C4)=O
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 (167.32 mM; ultrasonic and warming and heat to 60°C; 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 1.6732 mL 8.3660 mL 16.7319 mL
5 mM 0.3346 mL 1.6732 mL 3.3464 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 7.14 mg/mL (11.95 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 7.14 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (71.4 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% Corn Oil

    Solubility: 5 mg/mL (8.37 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL. 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 1.6732 mL 8.3660 mL 16.7319 mL 41.8298 mL
5 mM 0.3346 mL 1.6732 mL 3.3464 mL 8.3660 mL
10 mM 0.1673 mL 0.8366 mL 1.6732 mL 4.1830 mL
15 mM 0.1115 mL 0.5577 mL 1.1155 mL 2.7887 mL
20 mM 0.0837 mL 0.4183 mL 0.8366 mL 2.0915 mL
25 mM 0.0669 mL 0.3346 mL 0.6693 mL 1.6732 mL
30 mM 0.0558 mL 0.2789 mL 0.5577 mL 1.3943 mL
40 mM 0.0418 mL 0.2091 mL 0.4183 mL 1.0457 mL
50 mM 0.0335 mL 0.1673 mL 0.3346 mL 0.8366 mL
60 mM 0.0279 mL 0.1394 mL 0.2789 mL 0.6972 mL
80 mM 0.0209 mL 0.1046 mL 0.2091 mL 0.5229 mL
100 mM 0.0167 mL 0.0837 mL 0.1673 mL 0.4183 mL
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NXPZ-2 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:

NXPZ-22254492-08-3NXPZ2NXPZ 2Keap1-Nrf2Cortical neuronAlzheimer’s disease (AD)neurodegenerative diseaseKeap1-Nrf2 interactionoxidative stressInhibitorinhibitorinhibit

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