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Art. -Nr.: HY-187014

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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. Nr.: 141360-03-4
Formel: C₂₅H₃₅Cl₂F₃N₂O
Molecular Weight:507.46

Speicherung:

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

NNC 09-0026 Chemical Structure

CAS. Nr.: 141360-03-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[3]^[4]

N-type calcium channel

10-13 μM (IC₅₀)

L-type calcium channel

13 μM (IC₅₀)

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

In Vitro

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.

In Vivo

NNC 09-0026 (30 mg/kg; i.p.; 3 doses) provides 22% neuroprotection against ischaemia-induced neuronal death in the gerbil hippocampal CA1 region when administered 30 minutes before occlusion plus two follow-up doses, but fails to protect when dosing starts immediately after occlusion^[1].
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.

Animal Model:

Male Mongolian gerbils (≥3 months old, ≥60 g, 5-minute bilateral common carotid artery occlusion model)^[1]
Dosage:

30 mg/kg (pre-occlusion regimen); 30 mg/kg (post-occlusion regimen)
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)
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.

Animal Model:

Wistar (adult male)^[2]
Dosage:

0.1 mg/kg; 1.0 mg/kg; 10.0 mg/kg
Administration:

i.v.; single bolus
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).

Animal Model:

Fisher F-344 (adult male, 250-350 g)^[2]
Dosage:

30 mg/kg
Administration:

i.v.; slow infusion over 1 hour; beginning 30 minutes post-ischemia
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.

Animal Model:

Male Mongolian gerbils (at least 3 months old, 60-80 g, 5-minute bilateral common carotid artery occlusion)^[3]
Dosage:

30 mg/kg
Administration:

i.p.; 3 doses (30 minutes pre-occlusion, 24 hours post-occlusion, 48 hours post-occlusion)
Result:

Provided 22% neuroprotection against ischaemia-induced cell death in the CA1 region of the hippocampus.

Animal Model:

Focal cerebral ischemia rat model^[4]
Dosage:

30 mg/kg
Administration:

i.v.; single infusion over 1 h starting 30 min post-ischaemia
Result:

Reduced infarct volume in the focal ischaemia model.

Chemical Information

CAS. Nr. 141360-03-4
Molecular Weight 507.46
Formel C₂₅H₃₅Cl₂F₃N₂O
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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NNC 09-0026

Alle Calcium Channel Isoform-spezifische Produkte anzeigen