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.
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- CAS No.: 214348-10-4
- Formule: C29H34N4O3S
- Masse moléculaire:518.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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nNOS |
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.
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Cell Line:primary rat cortical neuron-glia cultures (12-14 days in vitro)
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Concentration:0.01 μM; 0.03 μM; 0.1 μM; 0.3 μM; 1 μM; 3 μM
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Incubation Time:24 h
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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.
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Cell Line:mouse hippocampal HT-22 cells
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Concentration:3 μM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.v.; single dose
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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).
Chemical Information
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CAS No. 214348-10-4
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Masse moléculaire 518.67
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Formule C29H34N4O3S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Demerlé-Pallardy C, et al. In vitro antioxidant neuroprotective activity of BN 80933, a dual inhibitor of neuronal nitric oxide synthase and lipid peroxidation. J Neurochem. 2000;74(5):2079-2086. [Content Brief]
[2]. Chabrier PE, et al. BN 80933, a dual inhibitor of neuronal nitric oxide synthase and lipid peroxidation: a promising neuroprotective strategy. Proc Natl Acad Sci U S A. 1999;96(19):10824-10829. [Content Brief]
[3]. Ding-Zhou L, et al. Neuroprotective effects of (S)-N-[4-[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)carbonyl]-1-piperazinyl]phenyl]-2-thiophenecarboximid-amide (BN 80933), an inhibitor of neuronal nitric-oxide synthase and an antioxidant, in model of transient focal cerebral ischemia in mice. J Pharmacol Exp Ther. 2003;306(2):588-594. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BN80933 Related Classifications
HY-183944 Related Classifications
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- BN80933
- 214348-10-4
- BN 80933
- BN-80933
- NO Synthase
- Reactive Oxygen Species (ROS)
- neuronal nitric oxide synthase
- hypoxia
- rat
- mouse hippocampal HT-22 cells
- middle cerebral artery occlusion
- cerebral cortex membrane homogenate
- primary rat cortical neuron-glia cultures
- buthionine sulfoximine
- glutamate
- lipid peroxidation
- Inhibitor
- inhibitor
- inhibit