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| Other Sizes |
| Targets |
7-Nitroindazole targets nitric oxide synthase (NOS), an enzyme responsible for the production of nitric oxide (NO) from L-arginine. It inhibits all three NOS isoforms (nNOS, eNOS, iNOS) in vitro, but shows functional selectivity for neuronal NOS (nNOS) in vivo. This selectivity is attributed to its ability to cross the blood-brain barrier and achieve higher concentrations in the central nervous system.
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| ln Vitro |
In vitro, 7-Nitroindazole inhibits NOS isoforms non-selectively with IC50 values of 0.71 µM for rat nNOS, 0.78 µM for bovine eNOS, and 5.8 µM for rat iNOS. It is used as a tool compound to study NOS function in cell-free systems. However, its in vitro profile does not reflect its in vivo selectivity.
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| ln Vivo |
In vivo, 7-Nitroindazole demonstrates selectivity for neuronal NOS (nNOS) due to its ability to cross the blood-brain barrier. It exhibits antinociceptive activity without increasing blood pressure, distinguishing it from non-selective NOS inhibitors like L-NAME that inhibit eNOS and cause hypertension. It is used to study the role of nNOS in pain, neurodegeneration, and other CNS conditions.
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| Enzyme Assay |
The in vitro enzyme assay for 7-Nitroindazole involves measuring the conversion of L-arginine to L-citrulline by NOS isoforms in the presence of the inhibitor. The IC50 values for nNOS, eNOS, and iNOS are determined by quantifying the reduction in enzyme activity. The assay uses purified enzymes or tissue homogenates and radiolabeled L-arginine.
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| Cell Assay |
In vitro cell-based assays for 7-Nitroindazole involve treating cells expressing NOS isoforms with the compound and measuring NO production (e.g., using the Griess assay for nitrite). The compound’s effects on NO-dependent signaling pathways in neuronal, endothelial, or immune cells can be evaluated.
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| Animal Protocol |
In vivo animal studies for 7-Nitroindazole involve administering the compound to rodents and measuring its effects on NOS activity in the brain, blood pressure, and nociceptive responses. It is used to study the role of nNOS in pain, cerebral ischemia, and neurodegenerative diseases. The compound is typically administered by intraperitoneal injection.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 7-Nitroindazole are not detailed in the provided literature. It is known to cross the blood-brain barrier, enabling its in vivo selectivity for nNOS. The compound has a crystalline solid appearance and solubility of >24.5 µg/mL at pH 7.4.
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| Toxicity/Toxicokinetics |
No specific toxicity data for 7-Nitroindazole are available in the provided literature. It is known to be a NOS inhibitor and should be handled with care. The compound is for research use only.
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| References |
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| Additional Infomation |
7-Nitroindazole is a research tool for studying NOS function. It shows in vivo selectivity for nNOS. It exhibits antinociceptive activity without increasing blood pressure. It is for research use only. Its CAS number is 2942-42-9.
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| Molecular Formula |
C7H5N3O2
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|---|---|
| Molecular Weight |
163.1335
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| Exact Mass |
163.038
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| CAS # |
2942-42-9
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| PubChem CID |
1893
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
211.2±23.0 °C at 760 mmHg
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| Melting Point |
185-186°C
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| Flash Point |
81.5±22.6 °C
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| Vapour Pressure |
0.2±0.4 mmHg at 25°C
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| Index of Refraction |
1.741
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| LogP |
1.42
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
12
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| Complexity |
192
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PQCAUHUKTBHUSA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H5N3O2/c11-10(12)6-3-1-2-5-4-8-9-7(5)6/h1-4H,(H,8,9)
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| Chemical Name |
7-nitro-1H-indazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~613.01 mM)
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.1301 mL | 30.6504 mL | 61.3008 mL | |
| 5 mM | 1.2260 mL | 6.1301 mL | 12.2602 mL | |
| 10 mM | 0.6130 mL | 3.0650 mL | 6.1301 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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