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

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.

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7-Nitroindazole Chemical Structure

7-Nitroindazole Chemical Structure

CAS No. : 2942-42-9

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Based on 1 publication(s) in Google Scholar

Other Forms of 7-Nitroindazole:

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1 Publications Citing Use of MCE 7-Nitroindazole

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Description

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

 

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]
In Vitro

7-Nitroindazole (0.01-100 μM) has obvious inhibitory effect on cerebellar NOS (IC50: 0.47 μM), and is more effective than L-NAME (HY-18729A) (IC50: 0.87 μM) and L-NMMA (HY-18732) (IC50: 2.37 μM)[1].

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

In Vivo

7-Nitroindazole (10-80 mg/kg; Intraperitoneal injection; Single dose) has an anti-injury and anti-nociceptive effect in a formalin-induced mouse pain model without increasing blood pressure[1].
7-Nitroindazole (25 mg/kg; Subcutaneous injection; 25 days) improves L-DOPA (HY-N0304)-induced dyskinesias in non-human primate models of Parkinson's disease[2].
7-Nitroindazole (5-20 mg/kg; Intraperitoneal injection; 6 weeks) improves the learning and memory of hypothyroidism rats[3].
7-Nitroindazole (30 mg/kg; Intraperitoneal injection; Single dose) enhances Fos immune response induced by muscle proprioceptive signaling within distinctive regions of the spinal cord in rats[4].

MedChemExpress (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.
Molecular Weight

163.14

Formula

C7H5N3O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=[N+](C1=CC=CC2=C1NN=C2)[O-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (612.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (15.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.04%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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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Product Name:
7-Nitroindazole
Cat. No.:
HY-69019
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