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 番号: 141360-03-4
- 分子式: C25H35Cl2F3N2O
- 分子量:507.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Calcium Channel アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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N-type calcium channel 10-13 μM (IC50) |
L-type calcium channel 13 μM (IC50) |
体外実験
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. Further protocols information, click here.
体内実験
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.
化学情報
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CAS 番号 141360-03-4
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分子量 507.46
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
NNC 09-0026 関連分類
HY-187014 関連分類
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Keywords
- 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