NADPH oxidase-IN-1   中文名称: NADPH氧化酶-抑制剂1

NOX2 1.9 μM (IC50) NOX4 2.47 μM (IC50)

通过平行人工膜通透性测定（PAMPA），NADPH氧化酶-IN-1（化合物11）的Pe值为13.6（10-6 cm/s），表明它可以穿过血脑屏障[1] 。在 BV2 小胶质细胞中，NADPH 氧化酶-IN-1（1 nM-10 mM；30 分钟）以剂量依赖性方式抑制 LPS 诱导的 ROS 产生 [1]。在 BV2 细胞中，促炎细胞因子 mRNA 表达受到 NADPH 氧化酶-IN-1（10 μM；24 小时）的抑制 [1]。此外，BV2 细胞的活化和迁移受到 NADPH 氧化酶-IN-1（1 nM-10 mM；24 小时）的抑制 [1]。

在帕金森病小鼠模型中，NADPH 氧化酶-IN-1（化合物 11）（30 mg/kg；口服；每日一次，持续 4 周）可减少多巴胺能神经元损失并减弱 MPTP 诱导的小胶质细胞活化 [1]。当通过静脉注射（10-300 mg/kg；单剂量）或灌胃（10-1000 mg/kg；单剂量）给药时，NADPH 氧化酶-IN-1 对雄性和雌性小鼠都是安全的[1]。大鼠药代动力学特征：参数 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 毫克/千克) 0.783 6.13 [0.67-2] 4.16 0.159 1.82 0.217 88.9

RT-PCR[1]
细胞类型： BV2 小胶质细胞
测试浓度： 10 μM
孵育时间： 24小时
实验结果：抑制BV2细胞中促炎细胞因子（iNOS、IL-1β、TNFα）的mRNA表达。

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细胞迁移测定 [1]
细胞类型： BV2 小胶质细胞
测试浓度： 10 μM
孵育持续时间：24 小时
实验结果：改善炎症反应和小胶质细胞迁移。

[1]. Shim S, et al. Discovery of a NADPH oxidase inhibitor,(E)-3-cyclohexyl-5-(4-((2-hydroxyethyl)(methyl) amino) benzylidene)-1-methyl-2-thioxoimidazolidin-4-oneone, as a novel therapeutic for Parkinson's disease[J]. European Journal of Medicinal Chemistry, 2022, 244: 114854.

C20H27N3O2S

373.51

2762405-17-2

O=C1/C(/N(C(N1C1CCCCC1)=S)C)=C\C1C=CC(=CC=1)N(C)CCO

DMSO: 62.5 mg/mL (167.33 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。