O-Desmethylcarvedilol
Based on 1 Customer Validation
O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 µM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively).
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- Pureza : 97.4%
- No. CAS: 72956-44-6
- Fòrmula: C23H24N2O4
- Peso molecular:392.45
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
7.62 μM
Compound: 9
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Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay
Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay
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[PMID: 24124794] |
Chemical Information
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No. CAS 72956-44-6
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Appearance Solid
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Peso molecular 392.45
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Fòrmula C23H24N2O4
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Color White to off-white
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SMILES
OC1=C(OCCNCC(COC2=CC=CC3=C2C4=C(C=CC=C4)N3)O)C=CC=C1
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Synonyms
Desmethylcarvedilol; BM-14242
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (269 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Chris D Smith, et al. Novel carvedilol analogues that suppress store-overload-induced Ca2+ release. J Med Chem. 2013 Nov 14;56(21):8626-55. [Content Brief]
[2]. K Strein, et al. Pharmacological profile of carvedilol, a compound with β-blocking and vasodilating properties. J Cardiovasc Pharmacol. 1987:10 Suppl 11:S33-41. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
O-Desmethylcarvedilol Related Classifications
HY-Z7733 Related Classifications
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