2. Immunology/Inflammation
  3. NO Synthase IFNAR
  4. nNOS-IN-2 trihydrochloride

nNOS-IN-2 trihydrochloride 是一种能穿透血脑屏障的一氧化氮合酶 (nNOS) 抑制剂。nNOS-IN-2 trihydrochloride 对人源和大鼠源 nNOS 的 Ki 值分别为 1.7 nM 和 2.3 nM，且对人源 eNOS 和 iNOS 表现出高选择性。nNOS-IN-2 trihydrochloride 还能在基础状态及 IFN-γ 暴露条件下有效降低人黑色素瘤细胞中 PD-L1 的表达。nNOS-IN-2 trihydrochloride 可用于研究黑色素瘤及相关信号通路。

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nNOS-IN-2 trihydrochloride

nNOS-IN-2 trihydrochloride Chemical Structure

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nNOS-IN-2 trihydrochloride 相关抗体

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nNOS iNOS eNOS

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways[1].
IC50 & Target

nNOS

1.7 nM (Ki, human nNOS)

nNOS

2.3 nM (Ki, rat nNOS)

体外研究
(In Vitro)

nNOS-IN-2 (compound 9) trihydrochloride 可在人黑色素瘤 A375 和 SK-MEL-28 细胞中诱导细胞毒性，EC50 值分别为 2.94 μM 和 2.08 μM，并且 nNOS-IN-2 trihydrochloride 比先导化合物 HH044 对人原代成纤维细胞的毒性更低[1]。
nNOS-IN-2 trihydrochloride (5 μM) 可将人黑色素瘤 A375 细胞中基础 PD-L1 表达水平降至对照组的 70%，且在 5 μM 浓度下能有效抑制 IFN-γ 诱导的 PD-L1 上调[1]。
nNOS-IN-2 trihydrochloride 可在 0.5 μM 的浓度下降低 HT22 细胞中谷氨酸诱导的 NO 积聚[1]。
nNOS-IN-2 trihydrochloride (200 μM; 17 h) 表现出中等血脑屏障通透性，在 200 μM 浓度下的有效通透性为 6.91×10-6 cm/s[1]。

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

nNOS-IN-2 trihydrochloride 相关抗体:

Western Blot Analysis[1]

Cell Line: human melanom A375
Concentration: 5 μM
Incubation Time: with 250 μg/mL IFN-γ
Result: Reduced basal PD-L1 expression levels in human melanoma A375 cells to 70% of the control group.
Effectively inhibited IFN-γ-induced PD-L1 upregulation at a concentration of 5 μM.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-last T1/2 Bioavailability CL C0 Vss
Mice[1] 3 mg/kg i.v. 0.08 h 87.68 ng/mL 500.82 11.27 h / 85.37 mL/min/kg 2477.24 ng/mL 49.55 L/kg
Mice[1] 10 mg/kg p.o. 0.50 h 14.46 ng/mL 128.81 20.16 h 8 % 2.61 mL/min/kg / /
分子量

533.92

Formula

C27H31Cl3N4O
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-2 trihydrochloride 相关分类

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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-2 trihydrochlorideNO SynthaseIFNARNitric oxide synthasesNOSInterferon-α/β receptorInterferon-alpha/beta receptorhuman melanoma A375 cellsmelanomaneuronal nitric oxide synthasePD-L1humanhuman melanoma cellsinterferon-gammaSK-MEL-28 cellsratblood-brain barrierInhibitorinhibitorinhibit

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