Dracoflavan B2
Dracoflavan B2 is an allosteric activator of pyruvate carboxylase (PC) that enhances Oxaloacetic acid (HY-W010382) production by inducing conformational changes in the BCCP domain, restores mitochondrial function, and improves metabolism, while also exhibiting anti-inflammatory activity. Dracoflavan B2 can be used for research on myocardial infarction.
For research use only. We do not sell to patients.
- CAS No.: 194794-47-3
- Formula: C33H30O7
- Molecular Weight:538.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Dracoflavan B2 (1.5-6 μM; 12 h) protects HUVECs against OGD-induced loss of viability, reduces LDH release in OGD-injured HUVECs, and increases cellular ATP levels in OGD-injured HUVECs in a concentration-dependent manner[1].
Dracoflavan B2 (1.5-6 μM; 12 h) improves the cell morphology and maintains the cell number of OGD-injured HUVECs[1].
Dracoflavan B2 exhibits stronger binding affinity for the PC-PT-CT-BCCP domain (Kd = 5.4 μM), whereas its binding affinity for the PC-BC domain is weaker (Kd = 41.2 μM)[1].
Dracoflavan B2 (0.01-200 μM) induces conformational changes in PC, manifested as a decrease in tryptophan fluorescence intensity[1].
Dracoflavan B2 (30-60 μM) specifically and dose-dependently competes with AD-DB2 for protein binding in cell lysates[1].
Dracoflavan B2 (compound 1b) is separated into a single diastereomer by chiral HPLC with a retention time of 13.2 min[2].
Dracoflavan B2 (1.5-6 μM; 12 h) inhibits OGD-induced apoptosis in HUVECs[1].
Dracoflavan B2 (6 μM; 12 h) inhibits apoptosis in HUVECs subjected to OGD[1].
Dracoflavan B2 (6 μM; 12 h) specifically restores mitochondrial number and area in OGD-injured HUVECs[1].
Dracoflavan B2 (6 μM; 12 h) restores the OGD-induced decrease in mitochondrial membrane potential in HUVECs and reduces mitochondrial reactive oxygen species levels[1].
Dracoflavan B2 (6 μM; 12 h) protects mitochondrial structural integrity in OGD-injured HUVECs[1].
Dracoflavan B2 (30 μM; 2 h) increases the thermal stability of pyruvate carboxylase in HUVECs[1].
Dracoflavan B2 (50-400 μM; 1 h) protects pyruvate carboxylase from proteolysis in HUVEC lysates in a concentration-dependent manner[1].
Dracoflavan B2 (30-60 μM; 4 h) competitively blocks the binding of the AD-DB2 probe to pyruvate carboxylase in HUVECs[1].
Dracoflavan B2 (1.5-6 μM; 12 h) acts as an agonist to promote PC activity in OGD-injured HUVECs[1].
Dracoflavan B2 (6 μM; 12 h) restores the mitochondrial oxygen consumption rate in OGD-injured HUVECs[1].
Dracoflavan B2 (6 μM; 12 h) increases TCA cycle intermediate levels and decreases lactate levels in OGD-injured HUVECs[1].
Dracoflavan B2 (6 μM; 6 h OGD pretreatment + 9 h [13C6]-glucose incubation) enhances PC-dependent TCA cycle anaplerotic flux in OGD-injured HUVECs, as evidenced by an increase in [13C3]-Oxaloacetic acid (HY-W010382)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVECs
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Concentration:1.5, 3, 6 μM
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Incubation Time:12 h
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Result:Restored cell viability that was reduced by OGD injury in a concentration-dependent manner.
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Cell Line:HUVECs
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Concentration:1.5, 3, 6 μM
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Incubation Time:12 h
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Result:Attenuated OGD-induced cytotoxicity, leading to reduced LDH leakage.
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Cell Line:HUVECs
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Concentration:1.5, 3, 6 μM
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Incubation Time:12 h
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Result:Inhibited OGD-induced apoptosis, as indicated by reduced chromatin condensation and nuclear shrinkage.
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Cell Line:HUVECs
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Concentration:6 μM
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Incubation Time:12 h
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Result:Inhibited OGD-induced apoptosis as measured by flow cytometry.
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Cell Line:HUVECs with PC knockdown
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Concentration:1.5, 3, 6 μM
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Incubation Time:12 h
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Result:Failed to rescue the OGD-induced decrease in cell viability after PC knockdown.
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Cell Line:HUVECs with PC knockdown
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Concentration:1.5, 3, 6 μM
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Incubation Time:12 h
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Result:Failed to rescue the OGD-induced increase in LDH release after PC knockdown.
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Cell Line:HUVECs with PC knockdown
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Concentration:1.5, 3, 6 μM
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Incubation Time:12 h
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Result:Failed to protect against OGD-induced apoptosis after PC knockdown.
In Vivo
Dracoflavan B2 (10-20 mg/kg) alleviates myocardial infarction injury in mice by improving cardiac function metrics and reducing fibrosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, under 8 weeks, permanent ligation of the left anterior descending coronary artery)[1]
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Dosage:10-20 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Attenuated myocardial infarction-induced reductions in ejection fraction and fractional shortening.
Alleviated pathological increases in heart weight-to-body weight ratio and serum lactate dehydrogenase levels.
Significantly reduced infarct areas, collagen accumulation, and fibrosis.
Promoted endothelial cell survival and reduced myocardial apoptosis.
Enhanced cardiac PC enzyme activity.
Restored AMPK-PGC-1α-Sirt1 axis by reducing p-AMPK and increasing PGC-1α and Sirt1 expression.
Chemical Information
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CAS No. 194794-47-3
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Molecular Weight 538.59
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Formula C33H30O7
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SMILES
O[C@@H]1[C@@]2(C3=CC=CC=C3)OC4=C(C5=C(CC[C@@H](C6=CC=CC=C6)O5)C(OC)=C4)[C@@H]1C7=C(OC)C(C)=C(O)C=C7O2
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dracoflavan B2 Related Classifications
HY-N21583 Related Classifications
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