2. Metabolic Enzyme/Protease
  3. NADPH Oxidase
  4. NADPH oxidase-IN-1

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.

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NADPH oxidase-IN-1 Chemical Structure

NADPH oxidase-IN-1 Chemical Structure

CAS No. : 2762405-17-2

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Based on 1 publication(s) in Google Scholar

NADPH oxidase-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

NOX2

1.9 μM (IC50)

NOX4

2.47 μM (IC50)

In Vitro

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.

NADPH oxidase-IN-1 Related Antibodies

RT-PCR[1]

Cell Line: BV2 microglial cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Inhibited the mRNA expression of pro-inflammatory cytokines (iNOS, IL-1β, TNFα) in BV2 cells.

Cell Migration Assay [1]

Cell Line: BV2 microglial cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Ameliorated inflammatory response and migration of microglia.
In Vivo

NADPH oxidase-IN-1 (compound 11) (30 mg/kg; p.o.; daily for 4 wk) attenuates MPTP induced microglia activation and diminishes dopaminergic neuronal damage in Parkinson's disease (PD) mice model[1].
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.
Molecular Weight

373.51

Formula

C20H27N3O2S
CAS No.
Appearance

Solid

Color

Orange to red

SMILES

CN(C1=CC=C(C=C1)/C=C2C(N(C(N\2C)=S)C3CCCCC3)=O)CCO
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 : 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6773 mL 13.3865 mL 26.7730 mL
5 mM 0.5355 mL 2.6773 mL 5.3546 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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 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
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NADPH oxidase-IN-1 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:

NADPH oxidase-IN-12762405-17-2NADPH OxidaseNOXParkinson's diseaseBV2 microglial cellsInhibitorinhibitorinhibit

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