NNC 09-0026
NNC 09-0026 is a neuronal calcium channel inhibitor. NNC 09-0026 exhibits IC50 values of 10 μM and 13 μM against neuronal L-type voltage-gated calcium channels, and an IC50 value of 13 μM against rat neuronal N-type voltage-gated calcium channels, with higher selectivity for neuronal L-type channels over peripheral L-type channels. NNC 09-0026 inhibits voltage-dependent Ca2+ channel currents, blocks Ca2+ influx through neuronal L-type and N-type voltage-gated calcium channels, and reduces potassium-stimulated calcium uptake in rat cerebral cortex synaptosomes. NNC 09-0026 inhibits TTX-sensitive Na+ channel currents in rat cerebellar Purkinje neurons. NNC 09-0026 attenuates ischemia-induced neuronal death, infarct volume and neurological deficits in rat models of cerebral ischemia. NNC 09-0026 can be used for studies on global cerebral ischemia, focal ischemia and cerebral ischemia-related research.
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- CAS No.: 141360-03-4
- 화학식: C25H35Cl2F3N2O
- 분자량:507.46
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
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N-type calcium channel 10-13 μM (IC50) |
L-type calcium channel 13 μM (IC50) |
NNC 09-0026 (0.1-10 μg/mL; 30 min on ice, 6 min at 37°C) potently inhibits potassium-stimulated calcium uptake into rat cerebral cortex synaptosomes with an IC50 of 13 μM[2].
NNC 09-0026 (10 μM; at least 3 min) blocks voltage-operated calcium currents by 43% at 10 μM in cultured rat dorsal root ganglion cells, and acts on both L-type and N-type neuronal calcium channels[2].
NNC 09-0026 inhibits Nitrendipine (HY-B0424) binding with an IC50 of 10 μM, showing that it is not very active on peripheral calcium channels[2].
NNC 09-0026 (10 μM; 20 min) weakly inhibits calcium-dependent contractions in depolarized guinea pig taenia coli smooth muscle, producing a dose ratio of 3.5 at 10 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NNC 09-0026 (30 mg/kg; i.v.; slow infusion over 1 hour; beginning 30 minutes post-ischemia) provides significant neuroprotection in a rat focal ischemia model, reducing infarct volume by 44.7% and improving neurological deficits without causing side effects[2].
NNC 09-0026 (30 mg/kg; i.p.; 3 doses) provides 22% neuroprotection against ischaemia-induced CA1 hippocampal cell death in gerbils[3].
NNC 09-0026 (30 mg/kg; i.v.; single infusion over 1 h starting 30 min post-ischaemia) reduces infarct volume in a rat model of focal cerebral ischaemia[4].
NNC 09-0026 (0.1-10 mg/kg; i.v.; single bolus) produces mild, dose-dependent reductions in blood pressure and heart rate in healthy adult male Wistar rats, with significant effects only at the 10.0 mg/kg i.v. bolus dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Mongolian gerbils (≥3 months old, ≥60 g, 5-minute bilateral common carotid artery occlusion model)[1]
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Dosage:30 mg/kg (pre-occlusion regimen); 30 mg/kg (post-occlusion regimen)
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Administration:i.p.; 3 doses (30 minutes pre-occlusion, 24h post-occlusion, 48h post-occlusion); i.p.; 3 doses (immediately post-occlusion, 24h post-occlusion, 48h post-occlusion)
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Result:Achieved 44 viable cells per 1 mm of CA1 hippocampus, corresponding to 22% neuroprotection when administered 30 minutes before occlusion.
Failed to provide neuroprotection, with viable cell counts (10 viable cells per 1 mm of CA1 hippocampus) not significantly different from ischaemic controls when administered immediately after occlusion.
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Animal Model:Wistar (adult male)[2]
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Dosage:0.1 mg/kg; 1.0 mg/kg; 10.0 mg/kg
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Administration:i.v.; single bolus
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Result:Caused a 0.5% peak decrease in blood pressure and 1.5% peak decrease in heart rate from basal levels.
Caused a 2.2% peak decrease in blood pressure and 2.6% peak decrease in heart rate from basal levels.
Caused a significant 28.3% peak decrease in blood pressure and 12.1% peak decrease in heart rate from basal levels (p < 0.01).
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Animal Model:Fisher F-344 (adult male, 250-350 g)[2]
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Dosage:30 mg/kg
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Administration:i.v.; slow infusion over 1 hour; beginning 30 minutes post-ischemia
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Result:Reduced hemispheric infarct by 43.1% and infarct volume by 44.7% (p < 0.05) compared to vehicle controls.
Significantly reduced abnormal neurological grade at 24 hours post-ischemia (p < 0.05).
Did not affect hemispheric swelling or cause overt neurobehavioral side effects.
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Animal Model:Male Mongolian gerbils (at least 3 months old, 60-80 g, 5-minute bilateral common carotid artery occlusion)[3]
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Dosage:30 mg/kg
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Administration:i.p.; 3 doses (30 minutes pre-occlusion, 24 hours post-occlusion, 48 hours post-occlusion)
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Result:Provided 22% neuroprotection against ischaemia-induced cell death in the CA1 region of the hippocampus.
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Animal Model:Focal cerebral ischemia rat model[4]
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Dosage:30 mg/kg
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Administration:i.v.; single infusion over 1 h starting 30 min post-ischaemia
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Result:Reduced infarct volume in the focal ischaemia model.
Chemical Information
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CAS No. 141360-03-4
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분자량 507.46
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화학식 C25H35Cl2F3N2O
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SMILES
FC(F)(F)C(C=C1)=CC=C1OC[C@H]2[C@H](C3=CC=C(C=C3)N(C)C)CCN(C2)CCCC.Cl.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. O'Neill MJ, et al. Effects of Ca2+ and Na+ channel inhibitors in vitro and in global cerebral ischaemia in vivo. Eur J Pharmacol. 1997 Aug 6;332(2):121-31. [Content Brief]
[2]. Barone FC, et al. Pharmacological profile of a novel neuronal calcium channel blocker includes reduced cerebral damage and neurological deficits in rat focal ischemia. Pharmacol Biochem Behav. 1994 May;48(1):77-85. [Content Brief]
[3]. Hicks CA, et al. Neuroprotective effects of the neuronal Ca(2+) channel blockers, LY042826 and LY393615 in vivo. European journal of pharmacology. 2000 Nov 24;408(3):241-8. [Content Brief]
[4]. O'Neill MJ, et al. LY393615, a novel neuronal Ca(2+) and Na(+) channel blocker with neuroprotective effects in models of in vitro and in vivo cerebral ischemia. Brain research. 2001 Jan 05;888(1):138-149. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NNC 09-0026 Related Classifications
HY-187014 Related Classifications
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- NNC 09-0026
- 141360-03-4
- Calcium Channel
- rat cerebellar Purkinje neurones
- healthy adult male Wistar rats
- rat neuronal N-type voltage-operated calcium channels
- neuronal L-type voltage-operated calcium channels
- rat focal ischemia model
- guinea pig taenia coli smooth muscle
- cultured rat dorsal root ganglion cells
- gerbil hippocampal CA1 region
- rat cerebral cortex synaptosomes
- rat models of cerebral ischaemia
- Inhibitor
- inhibitor
- inhibit