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Carvedilol

SKU: orb2893745

Description

Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.

Research Area

Cardiovascular Research, Cell Biology, Infectious Disease & Virology, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

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Carvedilol

Key Properties

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CAS Number72956-09-3
MW406.47
Purity99.73% (May vary between batches)
FormulaC24H26N2O4
SMILESCOC1=CC=CC=C1OCCNCC(O)COC1=C2C(NC3=C2C=CC=C3)=CC=C1
TargetAdrenergic Receptor,Autophagy,VEGFR,Antibacterial
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.92 mM);Ethanol:20.3 mg/mL (49.94 mM);DMSO:40.6 mg/mL (99.88 mM)

Bioactivity

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Target IC50
LDL oxidation:3.8 μM|β/α1-adrenoceptor:3.8 μM
In Vitro
Carvedilol rapidly inhibits Fe(++)-initiated lipid peroxidation, measured as thiobarbituric acid reactive substance (TBARS), in rat brain homogenate with an IC50 of 8.1 mM. Carvedilol protects against Fe(++)-induced alpha-tocopherol depletion in rat brain homogenate with an IC50 of 17.6 mM. Carvedilol dose-dependently decreases the intensity of the DMPO-OH signal with an IC50 of 25 mM. Carvedilol has inverse efficacy for stimulating G(s)-dependent adenylyl cyclase but stimulates phosphorylation of the receptor's cytoplasmic tail on previously documented G protein-coupled receptor kinase sites in beta2 adrenergic receptor (beta2AR)-expressing HEK-293 cells. Carvedilol (0.1-10 mM) produces a concentration-dependent inhibition of the mitogenesis stimulated by platelet-derived growth factor, epidermal growth factor, thrombin, and serum in human cultured pulmonary artery vascular smooth muscle cells, with IC50 values ranging from 0.3 mM to 2.0 mM. Carvedilol also produces a concentration-dependent inhibition of vascular smooth muscle cell migration induced by platelet-derived growth factor, with an IC50 value of 3 mM. Carvedilol decreases the extent of cellular vacuolization in cardiac myocytes and prevents the inhibitory effect of doxorubicin on mitochondrial respiration in both heart and liver. Carvedilol also prevents the decrease in mitochondrial Ca(2+) loading capacity and the inhibition of the respiratory complexes of heart mitochondria caused by doxorubicin.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Potassium Channel, peroxidation, SKF 105517, Vcam, VEGFR, β/α-1, inhibit, Inhibitor, lipid, inflammasome, NADPH, NLRP3, heart, LDL, HIF, failure, E-selectin, Adrenergic Receptor, blocker, BM 14190, BM14190, BM-14190, Autophagy, antihypertensive, angina, Carvedilol, Beta Receptor, congestive

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Quality Guarantee

Quality Guarantee

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Compound Identifiers

PubChem CID
2585 ↗

Key Properties

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No computed properties available.

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Carvedilol (orb2893745)

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% DMSO +
%+
% Tween 80 +
%

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50 mg
$ 70.00
100 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 90.00
500 mg
$ 140.00
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