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.
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. Further protocols information, click here.
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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.
Protocols
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Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)