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:
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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. Further protocols information, click here.
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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.
In Vivo
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.
Protocole
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
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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Keywords
- 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