An alkaloid with diverse biological activities; ERG channel blocker (IC50 = 19.7 μM using whole-cell patch-clamp electrophysiology in HEK293 cells expressing the human receptor); increases the amount and rate of calcium release from intracellular stores in healthy neonatal rat cardiac myocytes and those isolated from adult rats with heart failure in a concentration-dependent manner; increases expression of Ryr2 and Serca2a and decreases expression of Ncx; reduces mortality and improves cardiac function in a rat model of congestive heart failure; inhibits doxorubicin-induced myocardial apoptosis and mitochondrial cytochrome C release in mice when preadministered at a dose of 1mg/kg per day for four days; induces cellular autophagy and inhibits growth of MCF-7 breast cancer cells and induces mitochondrial apoptosis in MGC803 and MKN26 gastric cancer cells

Cyclovirobuxine D – 5 mg

Brand:
Cayman
CAS:
860-79-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Cyclovirobuxine D (CVB-D) is an alkaloid, and the main active component of the traditional Chinese medicine B. microphylla, that has diverse biological activities.{41280,41281,41282,41283,41284,41285} It is an ether-a-go-go related gene (ERG) potassium channel blocker with an IC50 value of 19.7 μM using whole-cell patch-clamp electrophysiology in HEK293 cells expressing the human receptor.{41280} IERG blockade is activation-dependent, indicating CVB-D binds to open ERG channels. CVB-D increases the amount and rate of calcium release from intracellular stores in healthy neonatal rat cardiac myocytes and those isolated from adult rats with heart failure in a concentration-dependent manner.{41281} It also increases expression of ryanodine receptor 2 (Ryr2) and sarcoplasmic reticulum calcium ATPase 2a (Serca2a) and decreases expression of the sodium-calcium exchanger (Ncx). In vivo, CVB-D (0.5-2.0 mg/kg) reduces mortality and improves cardiac function in a rat model of congestive heart failure.{41282} CVB-D pretreatment (1 mg/kg per day for 4 days) inhibits myocardial apoptosis and mitochondrial cytochrome C release induced by doxorubicin (Item No. 15007) in mice.{41283} CVB-D also induces cellular autophagy and inhibits growth of MCF-7 breast cancer cells and induces mitochondrial apoptosis in MGC803 and MKN26 gastric cancer cells.{41284,41285}  

 

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An alkaloid with diverse biological activities; ERG channel blocker (IC50 = 19.7 μM using whole-cell patch-clamp electrophysiology in HEK293 cells expressing the human receptor); increases the amount and rate of calcium release from intracellular stores in healthy neonatal rat cardiac myocytes and those isolated from adult rats with heart failure in a concentration-dependent manner; increases expression of Ryr2 and Serca2a and decreases expression of Ncx; reduces mortality and improves cardiac function in a rat model of congestive heart failure; inhibits doxorubicin-induced myocardial apoptosis and mitochondrial cytochrome C release in mice when preadministered at a dose of 1mg/kg per day for four days; induces cellular autophagy and inhibits growth of MCF-7 breast cancer cells and induces mitochondrial apoptosis in MGC803 and MKN26 gastric cancer cells

Formal name: (3β,5α,16α,20S)-4,4,14-trimethyl-3,20-bis(methylamino)-9,19-cyclopregnan-16-ol

Synonyms:  CVB-D|NSC 91722

Molecular weight: 402.7

CAS: 860-79-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Natural Products|Alkaloids||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure

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