Nexinhib20
Based on 1 publication(s) in Google Scholar
Nexinhib20 is an inhibitor that targets the interactions of Rab27a-JFC1 (IC50: 2.6 μM) and Rac-1-GTP. Nexinhib20 can inhibit neutrophil exocytosis, adhesion, and β2 integrin activation, and has anti-inflammatory activity. Nexinhib20 can be used in the research of diseases such as systemic inflammation and myocardial ischemia-reperfusion injury.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.86%
- CAS. Nr.: 331949-35-0
- Formel: C15H16N4O3
- Molecular Weight:300.31
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Nexinhib20
More
Biologische Aktivität
IC50: 2.6 μM (Rab27a-JFC1 interaction)[1]
Nexinhib20 (10 μM; 1 h) can inhibit the secretion of myeloperoxidase, the production of superoxide anions, and also inhibit the upregulation of adhesion molecules and receptors, such as CD11b and CD66b in neutrophils[1].
Nexinhib20 (10 μM; 1 h) can inhibit the IL-8-induced adhesion of human neutrophils to P-selectin and ICAM-1, the exocytosis and activation of β2 integrin, as well as the intracellular calcium flux and the activation of Rac-1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice with ischemia-reperfusion injury[2]
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Dosage:100 mM; 10 μL
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Administration:Intraperitoneal injection (i.p.); single dose
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Result:Significantly decreased infarct size (white area in the TTC-phthalo-blue-staining) after myocardial I/R injury.
Limited neutrophil recruitment to the coronary artery.
Improved left ventricular function.
Chemical Information
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CAS. Nr. 331949-35-0
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Appearance Solid
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Molecular Weight 300.31
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Formel C15H16N4O3
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Color White to yellow
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SMILES
O=C(/C(N1N=CN=C1)=C/C2=CC=CC([N+]([O-])=O)=C2)C(C)(C)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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JCI Insight
The CHI3L1-neutrophil axis drives immune suppression and breast cancer metastatic dissemination. [Abstract]2026 Feb 3:e199307. PMID: 41632530
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (332.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.32 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.32 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- 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)
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Handling Instructions (2659 KB)
Verweise
[1]. Johnson JL, et al. Identification of Neutrophil Exocytosis Inhibitors (Nexinhibs), Small Molecule Inhibitors of Neutrophil Exocytosis and Inflammation: DRUGGABILITY OF THE SMALL GTPase Rab27a. J Biol Chem. 2016 Dec 9;291(50):25965-25982. [Content Brief]
[2]. Liu W, et al. Nexinhib20 Inhibits Neutrophil Adhesion and β2 Integrin Activation by Antagonizing Rac-1-Guanosine 5'-Triphosphate Interaction. J Immunol. 2022 Oct 15;209(8):1574-1585. [Content Brief]
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 | 3.3299 mL | 16.6495 mL | 33.2989 mL | 83.2473 mL |
| 5 mM | 0.6660 mL | 3.3299 mL | 6.6598 mL | 16.6495 mL | |
| 10 mM | 0.3330 mL | 1.6649 mL | 3.3299 mL | 8.3247 mL | |
| 15 mM | 0.2220 mL | 1.1100 mL | 2.2199 mL | 5.5498 mL | |
| 20 mM | 0.1665 mL | 0.8325 mL | 1.6649 mL | 4.1624 mL | |
| 25 mM | 0.1332 mL | 0.6660 mL | 1.3320 mL | 3.3299 mL | |
| 30 mM | 0.1110 mL | 0.5550 mL | 1.1100 mL | 2.7749 mL | |
| 40 mM | 0.0832 mL | 0.4162 mL | 0.8325 mL | 2.0812 mL | |
| 50 mM | 0.0666 mL | 0.3330 mL | 0.6660 mL | 1.6649 mL | |
| 60 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3875 mL | |
| 80 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0406 mL | |
| 100 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8325 mL |
Nexinhib20 Related Classifications
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