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).
For research use only. We do not sell to patients.
- Purity: 97.4%
- CAS No.: 72956-44-6
- Formula: C23H24N2O4
- Molecular Weight:392.45
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Calcium Channel Isoforms
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
7.62 μM
Compound: 9
|
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
|
[PMID: 24124794] |
Chemical Information
-
CAS No. 72956-44-6
-
Appearance Solid
-
Molecular Weight 392.45
-
Formula C23H24N2O4
-
Color White to off-white
-
SMILES
OC1=C(OCCNCC(COC2=CC=CC3=C2C4=C(C=CC=C4)N3)O)C=CC=C1
-
Synonyms
Desmethylcarvedilol; BM-14242
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
-
Data Sheet (269 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[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)