Declopramide hydrochloride
Declopramide (3-Chloroprocainamide) hydrochloride is an orally active, blood-brain barrier-permeable IκBβ/NF-κB inhibitor and chemosensitizer. Declopramide exhibits affinity for rabbit 5-HT3 receptors (5-HT3R) with a Ki value of 3.2 μM. Declopramide inhibits IκBβ degradation, blocks NFκB activation, and induces rapid apoptosis and DNA strand breaks in cancer cells. Declopramide enhances the cytotoxicity induced by Cisplatin (HY-17394) and is also metabolically converted to N-acetyl declopramide. Declopramide can be used in the research of tumors such as brain astrocytoma.
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- CAS. Nr.: 52423-57-1
- Formel: C13H21Cl2N3O
- Molecular Weight:306.23
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Declopramide (250-1000 µM; 20 h) hydrochloride induces dose-dependent caspase-mediated early apoptosis in 70Z/3 mouse pre-B cells[1].
Declopramide (250-1000 µM; 24 h) hydrochloride inhibits LPS (HY-D1056)-induced activation of NF-κB in 70Z/3 mouse pre-B cells[1].
Declopramide inhibits the growth of HL60 and K562 leukemia cells in vitro, but its activity is weaker than that of its metabolite N-acetyl-declopramide[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine pre-B-cell line 70Z/3
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Concentration:250 µM; 500 µM; 1000 µM; 500 µM (with 1 h ZVADfmk pretreatment)
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Incubation Time:20 h; 17 h (with 1 h ZVADfmk pretreatment)
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Result:Induced a dose-dependent increase in early apoptosis (Annexin V-positive/7AAD-negative cells) and corresponding decrease in viable (7AAD-negative) cells in 70Z/3 cells.
Reduced viable cell percentage and increased early apoptotic cell percentage relative to untreated cells at 500 µM.
Significantly reduced declopramide-induced apoptosis when caspase inhibitor ZVADfmk was used, measured via both 7AAD and Annexin V staining.
Declopramide (25-200 mg/kg; i.m., p.o.; single dose) hydrochloride does not induce central nervous system-related sedative side effects in female Wistar-Furth rats[3].
Declopramide (25 mg/kg; i.m., p.o.; single dose) hydrochloride distributes to the brain, spleen and tumor tissues in scid mice bearing H2981 xenografts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (xenografted with human T24 brain astrocytoma cells)[2]
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Dosage:40 mg/kg
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Administration:p.o.; 3 doses at 0, 24, and 48 hours
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Result:Exhibited equivalent in vivo tumor growth inhibitory efficacy to intramuscularly administered 40 mg/kg declopramide.
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Animal Model:Wistar-Furth (female, 2 months old, ~200 g)[3]
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Dosage:25 mg/kg; 200 mg/kg
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Administration:i.m.; single dose; p.o.; single dose
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Result:Showed no observable sedative side effects or notable symptoms across all tested doses and observation periods.
Detected no significant differences in tunnel travel time between declopramide-treated rats and control rats at any dosage, administration route, or time point.
Chemical Information
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CAS. Nr. 52423-57-1
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Molecular Weight 306.23
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Formel C13H21Cl2N3O
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SMILES
O=C(C1=CC=C(C(Cl)=C1)N)NCCN(CC)CC.Cl
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Synonyms
3-Chloroprocainamide hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Declopramide hydrochloride Related Classifications
HY-111193A Related Classifications
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