A cardiac glycoside; inhibits human recombinant α1β1

Digitoxin – 250 mg

Brand:
Cayman
CAS:
71-63-6
Storage:
-20
UN-No:
- 2811 / 6.1

Digitoxin is a cardiac glycoside that has been found in Digitalis and has diverse biological activities.{29469,52442,52443,52444,52445} It inhibits human recombinant α1β1, α2β2, and α3β1 subunit-containing Na+/K+-ATPases with Ki values of 250, 63, and 136 nM, respectively.{29469} 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).{52442} 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 µM, respectively.{52443} 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.{52444} 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.{52445} Formulations containing digitoxin have previously been used in the treatment of congestive heart failure and cardiac arrhythmias.  

 

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Description

A cardiac glycoside; inhibits human recombinant α1β1, α2β2, and α3β1 subunit-containing Na+/K+-ATPases (Kis = 250, 63, and 136 nM, respectively); also inhibits hERG in HEK293 cells expressing hERG (IC50 = 11.1 nM); enhances developed tension and contractile force in electrically stimulated isolated guinea pig left atrial muscle at 0.2 and 0.4 µM, respectively; metabolized to digoxin in isolated rat liver microsomes; attenuates congestive heart failure and reduces myocardial hypertrophy in a rat model of myocardial infarction induced by coronary artery ligation at ~1 mg/kg per day); cytotoxic to a panel of 10 human cancer cell lines (IC50s = 12-76 nM)

Formal name: (3β,5β)-3-[(O-2,6-dideoxy-β-D-ribo-hexopyranosyl-(1→4)-O-2,6-dideoxy-β-D-ribo-hexopyranosyl-(1→4)-2,6-dideoxy-β-D-ribo-hexopyranosyl)oxy]-14-hydroxy-card-20(22)-enolide

Synonyms:  Digitoxoside|Lanatoxin|NSC 7529

Molecular weight: 765

CAS: 71-63-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Natural Products|Glycosides||Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Cell Death||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy

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