1. Immunology/Inflammation
  2. NO Synthase
  3. 7-Nitroindazole

7-Nitroindazole  (Synonyms: 7-硝基吲唑)

目录号: HY-69019 纯度: 99.04%
COA 产品使用指南

7-Nitroindazole 是一种具有选择性和能透过大脑屏障的一氧化氮合酶 (NOS) 抑制剂。7-Nitroindazole 能抑制中枢 NOS 活性,在小鼠小脑的 IC50 为 0.47 μM。7-Nitroindazole 具有抗伤害和神经保护的作用。

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7-Nitroindazole Chemical Structure

7-Nitroindazole Chemical Structure

CAS No. : 2942-42-9

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Other Forms of 7-Nitroindazole:

MCE 顾客使用本产品发表的 1 篇科研文献

查看 NO Synthase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

7-Nitroindazole is a selective and BBB-penatrable inhibitor of nitric oxide synthase (NOS). 7-Nitroindazole can inhibit the activity of central NOS with an IC50 of 0.47 μM in the cerebellum of mice. 7-Nitroindazole has anti-injurious and neuroprotective properties[1][2][3][4].

IC50 & Target

nNOS

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Astrocyte EC50
282.6 μM
Compound: 34
Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
[PMID: 17417631]
DLD-1 IC50
24 μM
Compound: 7-NI
Tested to inhibit the conversion of [3H]L-arginine to [3H]L-citrulline catalyzed by inducible NOS from human DLD-1 cells.
Tested to inhibit the conversion of [3H]L-arginine to [3H]L-citrulline catalyzed by inducible NOS from human DLD-1 cells.
10.1016/0960-894X(95)00273-V
J774 IC50
20 μM
Compound: 7-NI
Tested to inhibit the conversion of [3H]L-arginine to [3H]L-citrulline catalyzed by inducible NOS from mouse macrophage J774 cells
Tested to inhibit the conversion of [3H]L-arginine to [3H]L-citrulline catalyzed by inducible NOS from mouse macrophage J774 cells
10.1016/0960-894X(95)00273-V
RAW264.7 IC50
> 200 μM
Compound: 1
Inhibition of LPS and gamma-IFN-stimulated nitrite accumulation in mouse RAW 264.7 cells after 20 hrs
Inhibition of LPS and gamma-IFN-stimulated nitrite accumulation in mouse RAW 264.7 cells after 20 hrs
[PMID: 18502134]
体外研究
(In Vitro)

7-Nitroindazole (0.01-100 μM) 对小鼠小脑 NOS 有明显的抑制作用 (IC50: 0.47 μM),比 L-NAME (HY-18729A) (IC50: 0.87 μM) 和 L-NMMA (HY-18732) (IC50: 2.37 μM) 更有效[1]

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

体内研究
(In Vivo)

7-Nitroindazole (10-80 mg/kg;腹腔注射;单剂量) 在福尔马林诱导的小鼠疼痛模型中具有抗伤害和抗疼痛的作用,但不升高血压[1]
7-Nitroindazole (25 mg/kg;皮下注射;25 天) 在非人灵长类帕金森模型中可改善左旋多巴 (HY-N0304) 诱导的运动障碍[2]
7-Nitroindazole (5-20 mg/kg;腹腔注射;6 周) 对甲状腺功能减退幼鼠的学习记忆有改善作用[3]
7-Nitroindazole (30 mg/kg;腹腔注射;单剂量) 在大鼠脊髓特殊区域内增强肌肉本体感觉信号诱导的 Fos 免疫反应[4]

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

Animal Model: Formalin treated male LACA mice (28-32 g)[1]
Dosage: 10, 25, 50 and 80 mg/kg
Administration: Intraperitoneal injection (i.p.); single dose
Result: Decreased mouse cerebellar NOS activity measured 15 min thereafter by over 55% at a dose of 25 mg/kg.
Inhibition of late phase Formalin-induced hindpaw licking without influencing the early phase response with an ED50 of 26.0 mg/kg.
Did not increase MAP over the 45 min experimental period.
Animal Model: MPTP (HY-15608) and Madopar treated adult male cynomolgus monkeys (3.8-4.5 kg)[2]
Dosage: 25 mg/kg
Administration: Subcutaneous injection (s.c.); 25 days
Result: Dramatically decreased the intensity and duration of the L-DOPA (HY-N0304) induced dyskinesias (LIDs), reducing the profile by more than 50%.
Did not affect the improvement of Parkinson's disease and significantly reduced LIDs.
Animal Model: Propylthiouracil (HY-B0346) treated male Wistar juvenile rats (20 days old)[3]
Dosage: 5, 10, and 20 mg/kg
Administration: Intraperitoneal injection (i.p.); 6 weeks
Result: Shortened the escape latency and traveled distance and spent less time and traveled less distance to reach the platform in morris water maze test.
Enhanced the spatial memory of the rats in morris water maze test.
Reduced the time spent in the dark box post shock and diminished the number of entries into the dark box at all times in passive avoidance learning test.
Improved thiol, SOD, CAT, thiol, and BDNF but attenuated MDA and NO metabolites in the brain.
Animal Model: Wistar rats (240-290 g)[4]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.); single dose
Result: Increased the total number of Fos-ir interneurons and motor neurons (per slice), and the greatest increases in the number of Fos-ir neurons were found in the L4 (+100%) and L5 (+105%) segments.
分子量

163.14

Formula

C7H5N3O2

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (612.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.1299 mL 30.6493 mL 61.2985 mL
5 mM 1.2260 mL 6.1299 mL 12.2597 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (15.32 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.04%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 6.1299 mL 30.6493 mL 61.2985 mL 153.2464 mL
5 mM 1.2260 mL 6.1299 mL 12.2597 mL 30.6493 mL
10 mM 0.6130 mL 3.0649 mL 6.1299 mL 15.3246 mL
15 mM 0.4087 mL 2.0433 mL 4.0866 mL 10.2164 mL
20 mM 0.3065 mL 1.5325 mL 3.0649 mL 7.6623 mL
25 mM 0.2452 mL 1.2260 mL 2.4519 mL 6.1299 mL
30 mM 0.2043 mL 1.0216 mL 2.0433 mL 5.1082 mL
40 mM 0.1532 mL 0.7662 mL 1.5325 mL 3.8312 mL
50 mM 0.1226 mL 0.6130 mL 1.2260 mL 3.0649 mL
60 mM 0.1022 mL 0.5108 mL 1.0216 mL 2.5541 mL
80 mM 0.0766 mL 0.3831 mL 0.7662 mL 1.9156 mL
100 mM 0.0613 mL 0.3065 mL 0.6130 mL 1.5325 mL
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产品名称:
7-Nitroindazole
目录号:
HY-69019
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