1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. NO Synthase Reactive Oxygen Species (ROS)
  3. BN80933

BN80933 is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a rat Ki of 0.92 μM. BN80933 inhibits lipid peroxidation, and blocks hypoxia-induced lactate dehydrogenase elevation and delayed 8-epiprostaglandin F2α elevation. BN80933 can be used for the research of stroke, and traumatic brain injury.

For research use only. We do not sell to patients.

BN80933

BN80933 Chemical Structure

CAS No. : 214348-10-4

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Description

BN80933 is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a rat Ki of 0.92 μM. BN80933 inhibits lipid peroxidation, and blocks hypoxia-induced lactate dehydrogenase elevation and delayed 8-epiprostaglandin F2α elevation. BN80933 can be used for the research of stroke, and traumatic brain injury[1][2][3].

IC50 & Target[1]

nNOS

 

In Vitro

BN80933 (0.01-3 μM; 24 h) potently protects primary rat cortical neuron-glia cultures from hypoxia-induced cell death with an IC50 of 0.15 μM[1].
BN80933 (24 h) potently protects mouse hippocampal HT-22 cells from BSO (HY-106376)-induced oxidative cell death with an IC50 of 0.06 μM[1].
BN80933 (24 h) potently protects mouse hippocampal HT-22 cells from Glutamate-induced oxidative cell death with an IC50 of 0.13 μM, and maintains protective efficacy when administered 6 h after glutamate exposure[1].
BN80933 potently inhibits iron-dependent lipid peroxidation in rat cerebral cortex membrane homogenate with an IC50 of 0.31 μM, a potency that correlates strongly with its neuroprotective activity[1].
BN80933 (3 μM; 24 h) prevents glutamate-induced 8-isoprostane production but does not reverse GSH depletion in mouse hippocampal HT-22 cells, indicating it acts downstream of GSH loss to inhibit oxidative lipid peroxidation[1].
BN80933 (15 min) potently and competitively inhibits rat cerebellum nNOS with a Ki of 0.92 μM[2].
BN80933 (45 min) potently inhibits iron-dependent lipid peroxidation in rat cerebral cortex membrane homogenate with an IC50 of 0.29 μM[2].

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

Cell Cytotoxicity Assay[1]

Cell Line: primary rat cortical neuron-glia cultures (12-14 days in vitro)
Concentration: 0.01 μM; 0.03 μM; 0.1 μM; 0.3 μM; 1 μM; 3 μM
Incubation Time: 24 h
Result: Completely prevented hypoxia-induced morphological neuronal injury and elevation of LDH activity at 3 μM.
Exhibited concentration-dependent effect on LDH release in the submicromolar range, with near-maximal protection at 0.3 μM and an IC50 value of 0.15 μM.

ELISA Assay[1]

Cell Line: mouse hippocampal HT-22 cells
Concentration: 3 μM
Incubation Time: 6 h (GSH measurement); 24 h (8-isoprostane measurement)
Result: Did not modify the glutamate-induced depletion of intracellular GSH levels measured 6 h after exposure.
Reduced glutamate-induced elevation of 8-isoprostane levels (from 807 pg/mL to 296 pg/mL) measured 24 h after exposure.
Did not affect GSH or 8-isoprostane levels in untreated control cells.
In Vivo

BN80933 (3-10 mg/kg; i.v.; single dose) provides significant neuroprotection in mice[3].

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

Animal Model: Swiss mice (male, 22 to 25 g, transient focal cerebral ischemia induced by 15-minute left middle cerebral artery occlusion via intraluminal filament technique followed by reperfusion)[3]
Dosage: 3 mg/kg; 10 mg/kg
Administration: i.v.; single dose
Result: Improved grip score to 26.8 s, reduced infarct volume by 31% to 62 mm3, reduced Evans blue extravasation by 75% to 1.7 μg/g tissue, reduced brain water content by 37% to 83.8%, and reduced myeloperoxidase activity by 56% to 0.064 U/g tissue at 24 hours post-ischemia (3 mg/kg).
Improved grip score to 23.1 s, reduced infarct volume by 36% to 58 mm3, reduced Evans blue extravasation by 42% to 4.0 μg/g tissue, and reduced myeloperoxidase activity by 45% to 0.078 U/g tissue at 24 hours post-ischemia (10 mg/kg).
Improved grip score to 21.9 s and reduced infarct volume by 31% to 51 mm3 at 48 hours post-ischemia (3 mg/kg).
Improved grip score to 22.4 s and reduced infarct volume by 26% to 55 mm3 at 48 hours post-ischemia (10 mg/kg).
Molecular Weight

518.67

Formula

C29H34N4O3S

CAS No.
SMILES

CC1=C2C(O[C@@](C)(CC2)C(N3CCN(C4=CC=C(C=C4)NC(C5=CC=CS5)=N)CC3)=O)=C(C(C)=C1O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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BN80933
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HY-183944
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