NADPH oxidase-IN-1

CAS: 2762405-17-2 货号: N649399 分子式: C20H27N3O2S 分子量: 373.51
有货
别名
NADPH 氧化酶-IN-1
储存条件
-20°C储存
运输条件
超低温运输
★
规格
库存
价格
数量
5mg
N649399-5mg
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¥1,500.90
10mg
N649399-10mg
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¥2,400.90
25mg
N649399-25mg
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¥4,800.90
50mg
N649399-50mg
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¥7,600.90
100mg
N649399-100mg
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¥12,000.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


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 IC 50 s 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

In Vitro

NADPH oxidase-IN-1 (compound 11) can cross cross the blood-brain barrier (BBB) with P e value of 13.6 (10 -6 cm/s), determined by parallel artificial membrane permeability assay (PAMPA assay). NADPH oxidase-IN-1 (1 nM-10 mM; 30 min) LPS-induced ROS generation in BV2 microglial cells in a dose-dependent manner. NADPH oxidase-IN-1 (10 μM; 24 h) inhibits the mRNA expression of pro-inflammatory cytokines in BV2 cells. NADPH oxidase-IN-1 (1 nM-10 mM; 24 h) also inhibits activation and migration of BV2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell 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 AssayCell 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 . 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 . Pharmacokinetic profile in rats Parameters C 0 (μg/mL) C max (μg/mL) t 1/2 (h) T max (h) AUC last (μg/h/mL) k e (1/h) V d (L) V d /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.

Form:Solid

IC50& Target:NOX2 1.9 μM (IC 50 ) NOX4 2.47 μM (IC 50 )

规格

别名
NADPH 氧化酶-IN-1
英文名称
NADPH oxidase-IN-1
生化机理
NADPH 氧化酶-IN-1 是一种口服活性 NADPH 氧化酶(Nox)抑制剂,与神经元炎症有关。NADPH 氧化酶-IN-1 可穿过血脑屏障(BBB),抑制 Nox2 和 Nox4,其 IC 50 s 分别为 1.9 μM 和 2.47 μM。NADPH 氧化酶
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
分子量
373.51

技术文档

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