Digitoxin
(Synonyms: 洋地黄毒苷) 目录号 : GC34013
A cardiac glycoside with diverse biological activities
Cas No.:71-63-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Digitoxin is a cardiac glycoside that has been found in Digitalis and has diverse biological activities.1,2,3,4,5 It inhibits human recombinant α1β1, α2β2, and α3β1 subunit-containing Na+/K+-ATPases with Ki values of 250, 63, and 136 nM, respectively.1 Digitoxin inhibits the human-ether-a-go-go (hERG) potassium channel, also known as Kv11.1, in HEK293 cells expressing hERG (IC50 = 11.1 nM).2 It enhances developed tension and contractile force in electrically stimulated isolated guinea pig left atrial muscle when used at concentrations of 0.2 and 0.4 ?M, respectively.3 Dietary administration of digitoxin (~1 mg/kg per day) attenuates congestive heart failure and reduces myocardial hypertrophy in a rat model of myocardial infarction induced by coronary artery ligation.4 Digitoxin is also cytotoxic to a panel of 10 human cancer cell lines, including myeloma, lymphoma, and leukemia cancer cells, with IC50 values ranging from 12 to 76 nM.5 Formulations containing digitoxin have previously been used in the treatment of congestive heart failure and cardiac arrhythmias.
1.Katz, A., Lifshitz, Y., Bab-Dinitz, E., et al.Selectivity of digitalis glycosides for isoforms of human Na,K-ATPaseJ. Biol. Chem.285(25)19582-19592(2010) 2.Wang, L., Wible, B.A., Wan, X., et al.Cardiac glycosides as novel inhibitors of human ether-a-go-go-related gene channel traffickingJ. Pharmacol. Exp. Ther.320(2)525-534(2007) 3.Temma, K., Akera, T., and Brody, T.M.Inotropic effects of digitoxin in solated guines-pig heart under conditions which alter contractionEur. J. Pharm.76(4)361-370(1981) 4.Picollo, C.T., dos Santos, A.A., Antonio, E.L., et al.Digitoxin attenuates heart failure, reduces myocardial hypertrophy, and preserves the calcium-binding proteins in infarcted ratsJ. Cardiovasc. Pharmacol. Ther.25(3)265-272(2019) 5.Johansson, S., Lindholm, P., Gullbo, J., et al.Cytotoxicity of digitoxin and related cardiac glycosides in human tumor cellsAnticancer Drugs12(5)475-483(2001)
| Cas No. | 71-63-6 | SDF | |
| 别名 | 洋地黄毒苷 | ||
| Canonical SMILES | C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O | ||
| 分子式 | C41H64O13 | 分子量 | 764.94 |
| 溶解度 | DMSO : ≥ 100 mg/mL (130.73 mM) | 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。 |
||
| 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 | 1.3073 mL | 6.5365 mL | 13.0729 mL |
| 5 mM | 0.2615 mL | 1.3073 mL | 2.6146 mL |
| 10 mM | 0.1307 mL | 0.6536 mL | 1.3073 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。
Digitoxin accumulation
Br J Clin Pharmacol 1982 Aug;14(2):225-9.PMID:7104174DOI:10.1111/j.1365-2125.1982.tb01966.x.
1 Nine healthy volunteers received single 1 mg intravenous doses of Digitoxin, following which serum Digitoxin concentrations were measured at multiple points in time over the next 14 days. 2 Mean kinetic variables for Digitoxin were: volume of distribution, 0.76 l/kg; elimination half-life, 8 days; total clearance, 0.049 ml min-1 kg-1. 3 After a drug-free interval of at least 4 months, subjects took 0.07 mg of oral Digitoxin daily for 28 consecutive days. Serum Digitoxin concentrations were measured during the period of dosage and in the 21 day post-dosage washout. 4 Digitoxin accumulation was slow, proceeding with a mean half-life (7.9 days) that was nearly identical to the single-dose half-life. However, the two were not significantly correlated. 5 Mean observed steady-state serum concentrations (15.4 ng/ml) also were nearly identical to those predicted from the single-dose study (15.3 ng/ml), but again the two were not significantly correlated. 6 Steady state is very slowly attained after initiation of maintenance therapy with Digitoxin. The kinetic data suggest that a loading dose on the average should be 12 times the maintenance dose.
Digitoxin as an anticancer agent with selectivity for cancer cells: possible mechanisms involved
Expert Opin Ther Targets 2007 Aug;11(8):1043-53.PMID:17665977DOI:10.1517/14728222.11.8.1043.
Accumulating preclinical and clinical data suggest that the cardiac drug Digitoxin might be used in cancer therapy. Recent reports have shown that Digitoxin can inhibit the growth and induce apoptosis in cancer cells at concentrations commonly found in the plasma of cardiac patients treated with this drug. Several mechanisms have been associated with the anticancer activity of Digitoxin, yet at present it is unknown why malignant cells are more susceptible to this cardiac glycoside than non-malignant cells. This report analyses the possible anticancer mechanisms of Digitoxin and proposes that the inhibition of glycolysis may be a key mechanism by which this natural product selectively targets cancer cells. Finally, whether or not there is enough evidence to support the clinical evaluation of Digitoxin in patients with cancer is discussed.
Accidental Digitoxin poisoning
Am J Dis Child 1976 Apr;130(4):425-7.PMID:1266828DOI:10.1001/archpedi.1976.02120050083016.
A healthy 141/2-month-old child ingested 1.5 mg of Digitoxin by accident. Digitoxin was wrongly identified as digoxin, the initial electrocardiogram was misinterpreted, and the vomiting was underestimated as an important symptom of toxicity. Symptoms persisted and the patient was hospitalized. Serial Digitoxin levels were obtained and correlated with ECG and clinical course. It appears that serial Digitoxin levels can be a useful adjunct in diagnosis, assessment of severity, and indication of recovery from Digitoxin poisoning. In each patient, it is imperative that ECG, pharmacologic, and clinical indicators of digitalis toxicity be accurately identified for proper assessment of severity and appropriate management.
Successful Treatment of Severe Digitoxin Intoxication with CytoSorb® Hemoadsorption
Blood Purif 2021;50(1):137-140.PMID:32937619DOI:10.1159/000510292.
While several intoxications can be successfully treated with specific antidotes, intoxications with the steroid glycoside Digitoxin still represent a major challenge. Besides conventional approaches, CytoSorb® hemoadsorption might be another treatment option. We report on an 81-year-old female patient treated in our intensive care unit (ICU) with severe Digitoxin intoxication, acute renal failure, and urinary tract infection (UTI). As physiological Digitoxin elimination kinetics are known to appear slow, and also in regard to the renal failure, the decision was made to initiate continuous renal replacement therapy combined with CytoSorb hemoadsorption. The patient was hemodynamically stabilized within the first 4 h of treatment and initially required catecholamines to be stopped within 24 h of treatment. Pre- and post-adsorber drug level measurements showed a rapid elimination of Digitoxin. Antibiotic treatment with piperacillin/tazobactam was initiated, and despite CytoSorb hemoadsorption therapy and its known potential to reduce plasma concentrations of several drugs, the UTI was successfully treated. After 3 days of CytoSorb treatment, Digitoxin plasma levels were stable and almost normalized, and no clinical signs of intoxication were present. Five days after presentation, the patient was transferred from the ICU in a stable condition. CytoSorb hemoadsorption may be an easily available, efficient, and less cost-intensive therapy option than treatment with the Fab fragment, which is the currently recommended therapy for digitalis intoxications. Therefore, the use of CytoSorb might represent an alternative treatment for life-threatening complications of Digitoxin intoxications.
Digitoxin-quinidine interaction: pharmacokinetic evaluation
Ann Intern Med 1980 Nov;93(5):698-701.PMID:7212478DOI:10.7326/0003-4819-93-5-698.
The effect of quinidine on Digitoxin single-dose pharmacokinetics was evaluated in five healthy adults. Blood was collected for 3 weeks, and a complete urine collection was obtained for 4 days, after a single intravenous dose of Digitoxin. The protocol was conducted once while each subject was taking oral quinidine, for 3 weeks, and then repeated 10 days after discontinuing quinidine treatment. Quinidine induced the following changes in Digitoxin pharmacokinetics: Elimination half-life was prolonged from 174 +/- 25 to 261 +/- 58 hours (p less than 0.02); total body clearance decreased from 1.54 +/- 0.40 to 1.09 +/- 0.31 mL/h . kg (p less than 0.05); renal clearance decreased from 0.65 +/- 0.07 to 0.46 +/- 0.17 mL/h . kg (p less than 0.05). Digitoxin volume of distribution and protein binding were unaltered by quinidine. Quinidine caused a rise in serum Digitoxin levels. Digitoxin total body clearance was decreased by quinidine to an extent comparable to that reported for digoxin; however, the mechanism of the interaction with the two digitalis glycosides may, in part, be different.