Art. -Nr.: HY-149010

NXPZ-2

Kundenbewertung

Based on 1 Customer Validation

NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a K_i 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.55%
CAS. Nr.: 2254492-08-3
Formel: C₂₇H₂₇N₅O₇S₂
Molecular Weight:597.66

Speicherung:

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

NXPZ-2 Chemical Structure

CAS. Nr.: 2254492-08-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

K_i: 95 nM (Keap 1); EC₅₀: 120 and 170 nM (Keap 1) ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Peritoneal macrophage	CC₅₀	>10 μM Compound: NXPZ-2	Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by CCK8 assay Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by CCK8 assay	[PMID: 34119834]
Peritoneal macrophage	CC₅₀	>100 μM Compound: NXPZ-2	Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by Cell Titer-Blue assay Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by Cell Titer-Blue assay	[PMID: 35687391]
Peritoneal macrophage	CC₅₀	>100 μM Compound: 1; NXPZ-2	Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability incubated for 24 hrs by Cell titer-blue assay Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability incubated for 24 hrs by Cell titer-blue assay	[PMID: 37257073]
Peritoneal macrophage	EC₅₀	1.12 μM Compound: NXPZ-2	Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as suppression of NO level pretreated with LPS followed by compound addition and measured after 24 hrs by Griess reagent based assay Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as suppression of NO level pretreated with LPS followed by compound addition and measured after 24 hrs by Griess reagent based assay	[PMID: 35687391]
Peritoneal macrophage	EC₅₀	1.4 μM Compound: NXPZ-2	Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as inhibition of TNF alpha level after 4 hrs by ELISA method Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as inhibition of TNF alpha level after 4 hrs by ELISA method	[PMID: 35687391]

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.

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].

Chemical Information

CAS. Nr. 2254492-08-3
Appearance Solid
Molecular Weight 597.66
Formel C₂₇H₂₇N₅O₇S₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

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

1.6732 mL

8.3660 mL

16.7319 mL

5 mM

0.3346 mL

1.6732 mL

3.3464 mL

10 mM

0.1673 mL

0.8366 mL

1.6732 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 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.

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:

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

Verweise

[1]. Yi Sun, et al. Direct inhibition of Keap1-Nrf2 Protein-Protein interaction as a potential therapeutic strategy for Alzheimer's disease. Bioorg Chem. 2020 Oct;103:104172. [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	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

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

NXPZ-2

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-Alzheimer's Disease Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NXPZ-2

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-Alzheimer's Disease Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NXPZ-2 Related Classifications

HY-149010 Related Classifications