Carvedilol-d5 |
Catalog No.GC47045 |
An internal standard for the quantification of carvedilol
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 929106-58-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Carvedilol-d5 is intended for use as an internal standard for the quantification of carvedilol by GC- or LC-MS. Carvedilol is a non-selective antagonist of the β-adrenergic receptor (β-AR; Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively).1 It also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively).2 Carvedilol reverses increases in heart rate induced by the β1-AR agonist isoproterenol in isolated guinea pig atria (Kb = 0.8 nM) and induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM).3 It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg.2 Carvedilol also inhibits the contractile response to the α1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM).3 It decreases systolic blood pressure and heart rate in rat models of hypertension, including spontaneously hypertensive, renal hypertensive, and deoxycorticosterone acetate-treated rats when administered at doses ranging from 3 to 30 mg/kg.4 Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation.5,6,7 Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.
1.Baker, J.G.The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptorsBr. J. Pharmacol.144(3)317-322(2005) 2.Groszek, G., Nowak-KrÓl, A., Wdowik, T., et al.Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2Eur. J. Med. Chem.44(12)5103-5111(2009) 3.Nichols, A.J., Sulpizio, A.C., Ashton, D.J., et al.In vitro pharmacologic profile of the novel beta-adrenoceptor antagonist and vasodilator, carvedilolPharmacology39(5)327-336(1989) 4.Tanaka, M., Masumura, H., Tanaka, S., et al.Studies on the antihypertensive properties of carvedilol, a compound with beta-blocking and vasodilating effectsJ. Cardiovasc. Pharmacol.10(Suppl 11)S52-S57(1987) 5.Wisler, J.W., DeWire, S.M., Whalen, E.J., et al.A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signalingProc. Natl. Acad. Sci. U.S.A.104(42)16657-16662(2007) 6.Kim, I.M., Tilley, D.G., Chen, J., et al.β-blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivationProc. Natl. Acad. Sci. U.S.A.105(38)14555-14560(2008) 7.Ibrahim, I.A.A.E.H., and Kurose, H.β-Arrestin-mediated signaling improves the efficacy of therapeuticsJ. Pharmacol. Sci.118(4)408-412(2012)
Cas No. | 929106-58-1 | SDF | |
Canonical SMILES | COC1=C(OCCNC([2H])([2H])C(C([2H])([2H])OC2=C(C(C=CC=C3)=C3N4)C4=CC=C2)([2H])O)C=CC=C1 | ||
Formula | C24H21D5N2O4 | M.Wt | 411.5 |
Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 5 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4301 mL | 12.1507 mL | 24.3013 mL |
5 mM | 0.486 mL | 2.4301 mL | 4.8603 mL |
10 mM | 0.243 mL | 1.2151 mL | 2.4301 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 38 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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