NADPH oxidase-IN-1
Based on 1 Customer Validation
NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 2762405-17-2
- Formula: C20H27N3O2S
- Molecular Weight:373.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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NOX2 1.9 μM (IC50) |
NOX4 2.47 μM (IC50) |
NADPH oxidase-IN-1 (compound 11) can cross cross the blood-brain barrier (BBB) with Pe value of 13.6 (10-6 cm/s), determined by parallel artificial membrane permeability assay (PAMPA assay)[1].
NADPH oxidase-IN-1 (1 nM-10 mM; 30 min) LPS-induced ROS generation in BV2 microglial cells in a dose-dependent manner[1].
NADPH oxidase-IN-1 (10 μM; 24 h) inhibits the mRNA expression of pro-inflammatory cytokines in BV2 cells[1].
NADPH oxidase-IN-1 (1 nM-10 mM; 24 h) also inhibits activation and migration of BV2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV2 microglial cells
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Inhibited the mRNA expression of pro-inflammatory cytokines (iNOS, IL-1β, TNFα) in BV2 cells.
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Cell Line:BV2 microglial cells
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Ameliorated inflammatory response and migration of microglia.
NADPH oxidase-IN-1 is safe in both male and female mice following IV injection (10-300 mg/kg; single dose) and oral gavage (10-1000 mg/kg; single dose), respectively[1].
Pharmacokinetic profile in rats
| Parameters | C0 (μg/mL) | Cmax (μg/mL) | t1/2 (h) | Tmax (h) | AUClast (μg/h/mL) | ke (1/h) | Vd (L) | Vd/F (L) | Cl (L/h) | Cl/F (L/h) | F (%) |
| IV (2 mg/kg) | 1.70 | 0.79 | 0.468 | 1.32 | 0.211 | 0.217 | |||||
| PO (10 mg/kg) | 0.609 | 5.01 | [0.083-2] | 1.31 | 0.170 | 1.99 | 0.341 | 56.0 | |||
| PO (20 mg/kg) | 0.783 | 6.13 | [0.67-2] | 4.16 | 0.159 | 1.82 | 0.217 | 88.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2762405-17-2
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Appearance Solid
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Molecular Weight 373.51
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Formula C20H27N3O2S
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Color Orange to red
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SMILES
CN(C1=CC=C(C=C1)/C=C2C(N(C(N\2C)=S)C3CCCCC3)=O)CCO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 62.5 mg/mL (167.33 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)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 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)
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 |
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| DMSO | 1 mM | 2.6773 mL | 13.3865 mL | 26.7730 mL | 66.9326 mL |
| 5 mM | 0.5355 mL | 2.6773 mL | 5.3546 mL | 13.3865 mL | |
| 10 mM | 0.2677 mL | 1.3387 mL | 2.6773 mL | 6.6933 mL | |
| 15 mM | 0.1785 mL | 0.8924 mL | 1.7849 mL | 4.4622 mL | |
| 20 mM | 0.1339 mL | 0.6693 mL | 1.3387 mL | 3.3466 mL | |
| 25 mM | 0.1071 mL | 0.5355 mL | 1.0709 mL | 2.6773 mL | |
| 30 mM | 0.0892 mL | 0.4462 mL | 0.8924 mL | 2.2311 mL | |
| 40 mM | 0.0669 mL | 0.3347 mL | 0.6693 mL | 1.6733 mL | |
| 50 mM | 0.0535 mL | 0.2677 mL | 0.5355 mL | 1.3387 mL | |
| 60 mM | 0.0446 mL | 0.2231 mL | 0.4462 mL | 1.1155 mL | |
| 80 mM | 0.0335 mL | 0.1673 mL | 0.3347 mL | 0.8367 mL | |
| 100 mM | 0.0268 mL | 0.1339 mL | 0.2677 mL | 0.6693 mL |
NADPH oxidase-IN-1 Related Classifications
HY-152026 Related Classifications
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