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

NADPH oxidase-IN-1 

Cat. No.: HY-152026
Handling Instructions

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.

NADPH oxidase-IN-1 Chemical Structure

NADPH oxidase-IN-1 Chemical Structure

CAS No. : 2762405-17-2

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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].

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

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

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

Molecular Weight

373.51

Formula

C20H27N3O2S

CAS No.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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NADPH oxidase-IN-1
Cat. No.:
HY-152026
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