| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
3-Bromo-7-nitroindazole primarily targets neuronal nitric oxide synthase (nNOS). It inhibits rat nNOS with an IC50 of 0.17 µM, bovine eNOS with an IC50 of 0.86 µM, and rat iNOS with an IC50 of 0.29 µM. This indicates that while it is a pan-NOS inhibitor, it exhibits approximately 5-fold selectivity for nNOS over eNOS and about 1.7-fold selectivity over iNOS.
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|---|---|
| ln Vitro |
In vitro, 3-Bromo-7-nitroindazole is a more potent inhibitor of nNOS than 7-nitroindazole. It potently inhibits rat nNOS with an IC50 of 0.17 µM. It also inhibits bovine eNOS (IC50 = 0.86 µM) and rat iNOS (IC50 = 0.29 µM). By inhibiting NOS enzymes, it reduces the synthesis of nitric oxide (NO), a key signaling molecule involved in neurotransmission, vasodilation, and immune function.
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| ln Vivo |
In vivo, 3-Bromo-7-nitroindazole affects nitric oxide (NO) synthesis throughout the body and brain. By inhibiting nNOS, it modulates NO-dependent signaling pathways in the central nervous system. It has been used in studies investigating the role of NO in neurodegeneration, pain, inflammation, and cognitive function. Its selectivity for nNOS over eNOS suggests it may have fewer cardiovascular side effects compared to non-selective NOS inhibitors.
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| Enzyme Assay |
In vitro enzyme assays for 3-Bromo-7-nitroindazole are conducted using recombinant or purified NOS enzymes (nNOS, eNOS, iNOS). Enzyme activity is measured by monitoring the conversion of L-arginine to L-citrulline using radiolabeled [³H]-L-arginine or by measuring nitrite production using the Griess reaction. The compound is incubated with the enzyme, substrate, and cofactors (NADPH, CaM, BH4) at varying concentrations, and IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for 3-Bromo-7-nitroindazole are performed using neuronal cell lines (e.g., SH-SY5Y, PC12) or primary neuronal cultures that express nNOS. Cells are treated with compound concentrations ranging from 0.01 to 10 µM for 1-24 hours. NO production is measured using fluorescent NO indicators such as DAF-FM DA or by quantifying nitrite in culture supernatants using the Griess reaction. Cell viability is assessed to evaluate cytotoxicity.
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| Animal Protocol |
In vivo animal studies for 3-Bromo-7-nitroindazole have been conducted in rodent models. Studies include behavioral models to assess the role of nNOS in anxiety, depression, and cognition. The compound is typically administered intraperitoneally or orally. Endpoints include behavioral assessments, tissue NO levels, and histopathological examination of brain regions. Dosages and administration routes vary depending on the specific experimental model.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 3-Bromo-7-nitroindazole are limited. The compound has a molecular weight of 242.03 and is soluble in DMSO (10 mM). Based on its physicochemical properties, it is expected to cross the blood-brain barrier due to its small size and moderate lipophilicity, which is desirable for nNOS inhibition in the central nervous system. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion.
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| Toxicity/Toxicokinetics |
Toxicological data for 3-Bromo-7-nitroindazole are limited. As a research compound, it is designated for laboratory use only. No significant acute toxicity has been reported. Standard toxicity screening would involve acute and repeated-dose studies in rodents with evaluation of clinical signs, body weight, hematology, clinical chemistry, and histopathology.
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| References | |
| Additional Infomation |
3-Bromo-7-nitroindazole is a potent and selective inhibitor of neuronal nitric oxide synthase (nNOS) with IC50 values of 0.17 µM for nNOS, 0.86 µM for eNOS, and 0.29 µM for iNOS. It is a more potent nNOS inhibitor than 7-nitroindazole. It affects NO synthesis throughout the body and brain. It is used as a research tool to study NO signaling in neurological disorders, inflammation, and cardiovascular function.
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| Molecular Formula |
C7H4BRN3O2
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|---|---|
| Molecular Weight |
242.0296
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| Exact Mass |
240.948
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| CAS # |
74209-34-0
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| PubChem CID |
1649
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| Appearance |
Light yellow to yellow solid powder
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| Density |
2.0±0.1 g/cm3
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| Boiling Point |
437.3±25.0 °C at 760 mmHg
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| Melting Point |
175-185 °C
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| Flash Point |
218.3±23.2 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.764
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| LogP |
2.52
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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 |
13
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| Complexity |
220
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NFSTZPMYAZRZPC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H4BrN3O2/c8-7-4-2-1-3-5(11(12)13)6(4)9-10-7/h1-3H,(H,9,10)
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| Chemical Name |
3-bromo-7-nitro-2H-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 (~413.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1317 mL | 20.6586 mL | 41.3172 mL | |
| 5 mM | 0.8263 mL | 4.1317 mL | 8.2634 mL | |
| 10 mM | 0.4132 mL | 2.0659 mL | 4.1317 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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