2. nNOS-IN-6

nNOS-IN-6 是一种人源神经元型一氧化氮合酶 (hnNOS) 抑制剂，其对人源 hnNOS 和大鼠 rnNOS 的 Ki 分别为 16 nM 和 34 nM。nNOS-IN-6 在 PAMPA-BBB 实验中表现出高有效通透性，且在小鼠体内药代动力学研究中显示出持续的全身暴露、低清除率和良好的脑穿透性。nNOS-IN-6 可用于神经退行性疾病、黑色素瘤的研究。

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nNOS-IN-6

nNOS-IN-6 Chemical Structure

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nNOS-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma[1].

体外研究
(In Vitro)

nNOS-IN-6 (compound 16) 可强效抑制人神经元型一氧化氮合酶 (hnNOS)，其 Ki 为 16 nM，且对人内皮型一氧化氮合酶 (heNOS) 的选择性约为 1800 倍，对人诱导型一氧化氮合酶 (hiNOS) 的选择性约为 2900 倍[1]。
nNOS-IN-6 (200 μM; 17 h) 在 PAMPA-BBB 实验中具有高有效渗透率 (13.04×10-6 cm/s)，显示出强大的中枢神经系统渗透潜力[1]。

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

nNOS-IN-6 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route C0/Cmax Tmax (Plasma) AUClast T1/2 Vss Bioavailability Cmax Tmax (Brain) CL
Mice[1] 3 mg/kg i.v. 654.08 ng/mL 0.083 h 654.03 ng·h/mL 2.49 h 16.08 L/kg / / / 74.6 mL/min/kg
Mice[1] 10 mg/kg p.o. 86.51 ng/mL 1.0 h 356.54 7.96 h 222.69 L/kg 16.4 % 172.0 ng/g 12.0 h /
体内研究
(In Vivo)

nNOS-IN-6 (3-10 mg/kg; i.v., p.o.; 单次) 在雄性 C57BL/6 小鼠中单次静脉和口服给药后，表现出高全身清除率、低口服生物利用度、大分布容积，以及延迟但可检测到的脑渗透[1]。

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

Animal Model: C57BL/6 mice (male)[1]
Dosage: 3 mg/kg (i.v.);
10 mg/kg (p.o.)
Administration: i.v.; single dose; p.o.; single dose
Result: Exhibited initial plasma concentration (C0) of 654.08 ng/mL at 0.083 h, AUClast of 654.03 h·ng/mL, terminal half-life (t1/2) of 2.49 h, systemic clearance of 74.6 mL/min/kg, steady-state volume of distribution (Vss) of 16.08 L/kg after intravenous administration.
Reached plasma Cmax of 86.51 ng/mL at 1.0 h, AUClast of 356.54 h·ng/mL, t1/2 of 7.96 h, Vss of 222.69 L/kg, oral bioavailability of 16.4% after oral administration.
Achieved brain Cmax of 172.0 ng/g at 12.0 h, brain-Kp (AUClast) of 24.0 after oral administration.
分子量

370.25

Formula

C17H18Cl2FN3O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

nNOS-IN-6 相关分类

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  • 稀释计算器

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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.

Keywords:

nNOS-IN-6human eNOSrat nNOSmale C57BL/6 micePAMPA-BBB assaysmousemelanomahuman neuronal nitric oxide synthasehuman iNOSneurodegenerative diseasesblood-brain barrierInhibitorinhibitorinhibit

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