Carvedilol-d5
(Synonyms: 卡维地洛-D5,BM 14190-d5) 目录号 : GC47045An internal standard for the quantification of carvedilol
Cas No.:929106-58-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- 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 | |
别名 | 卡维地洛-D5,BM 14190-d5 | ||
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 | ||
分子式 | C24H21D5N2O4 | 分子量 | 411.5 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 5 mg/ml | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。