| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
ABCB1 (P-glycoprotein, P-gp). Ganoderenic acid B acts by inhibiting the transport function of the ABCB1 efflux pump, which is frequently overexpressed in multidrug-resistant cancer cells. Importantly, mechanistic studies have revealed that this compound does not alter the expression level of ABCB1 nor does it affect the activity of ABCB1 ATPase. This suggests that Ganoderenic acid B functions as a direct inhibitor of the drug transport function rather than through modulation of protein expression or ATP hydrolysis, representing a distinct mechanism of action for reversing MDR.
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| ln Vitro |
Ganoderenic acid B exhibits a potent reversal effect on ABCB1-mediated multidrug resistance in HepG2/ADM hepatocellular carcinoma cells when co-administered with Doxorubicin. It significantly enhances the cytotoxicity of chemotherapeutics towards ABCB1-overexpressing MDR cancer cells by directly inhibiting the efflux function of the P-glycoprotein transporter. The compound does not affect ABCB1 expression levels or ATPase activity, indicating its role as a functional inhibitor of drug transport rather than a modulator of protein expression or enzymatic function.
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| ln Vivo |
While specific in vivo data for Ganoderenic acid B is limited in the available literature, its mechanism of action as an ABCB1 transport inhibitor suggests that it could potentially enhance the efficacy of chemotherapeutic agents in vivo by reversing MDR in tumor models. The compound's natural product origin and favorable physicochemical properties (LogP 2.39, molecular weight 514.65) may support oral bioavailability, though this has not been experimentally confirmed. Further in vivo studies would be required to validate its efficacy and pharmacokinetic profile.
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| Enzyme Assay |
In vitro receptor binding or functional assays for Ganoderenic acid B typically involve evaluating its interaction with ABCB1 using membrane preparations from drug-resistant cancer cells. Transport assays can be performed using fluorescent ABCB1 substrates (such as Rhodamine 123 or Calcein-AM) in the presence of increasing concentrations of the compound to measure its ability to inhibit P-gp-mediated efflux. ATPase activity assays can also be conducted to determine whether the compound affects the enzymatic function of ABCB1, which has been shown to be unaffected.
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| Cell Assay |
In vitro cellular assays for Ganoderenic acid B are typically performed using ABCB1-overexpressing cell lines such as HepG2/ADM, which are resistant to Doxorubicin. Cells are treated with increasing concentrations of Ganoderenic acid B in combination with a fixed concentration of Doxorubicin or other chemotherapeutic agents. Cell viability is then measured using MTT, CCK-8, or similar assays to determine the reversal of drug resistance. The compound's ability to enhance the cytotoxicity of chemotherapeutics in these resistant cell lines serves as the primary readout for its biological activity.
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| Animal Protocol |
Specific in vivo animal study protocols for Ganoderenic acid B are not well-documented in the available literature. However, for ABCB1 inhibitors, typical in vivo efficacy studies would involve the use of murine xenograft models bearing drug-resistant human tumor cells (e.g., HepG2/ADM). The test compound would be administered orally or intraperitoneally, alone or in combination with a chemotherapeutic agent such as Doxorubicin, to evaluate its ability to enhance antitumor efficacy and reverse MDR in vivo. Tumor volume, body weight, and survival would be monitored as primary endpoints.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Ganoderenic acid B are not extensively reported in the available literature. The compound has a molecular weight of 514.65 and a LogP of 2.39, suggesting moderate lipophilicity that may support oral absorption. It is supplied as a white to off-white solid powder and is soluble in DMSO (100 mg/mL). The compound should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years, and in solvent at -80°C for 6 months or at -20°C for 1 month, protected from moisture and light.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for Ganoderenic acid B in the published literature. As a natural triterpenoid from Ganoderma lucidum, it is generally considered to have a favorable safety profile, though this has not been systematically evaluated in preclinical toxicology studies. The compound is intended for research use only and is not for human therapeutic applications. Standard safety precautions should be observed when handling this research compound.
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| References | |
| Additional Infomation |
Ganoderenic acid B is a lanostane-type triterpene with the molecular formula C30H42O7 and a molecular weight of 514.65. Its IUPAC name is (E)-6-[(3S,5R,7S,10S,13R,14R,17R)-3,7-dihydroxy-4,4,10,13,14-pentamethyl-11,15-dioxo-2,3,5,6,7,12,16,17-octahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methyl-4-oxohept-5-enoic acid. The compound is isolated from Ganoderma lucidum and exhibits potent reversal of ABCB1-mediated multidrug resistance. It is a research tool for studying P-glycoprotein function and MDR reversal strategies in cancer.
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| Molecular Formula |
C30H42O7
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|---|---|
| Molecular Weight |
514.65
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| Exact Mass |
514.293
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| CAS # |
100665-41-6
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| PubChem CID |
71457627
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
702.7±60.0 °C at 760 mmHg
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| Flash Point |
392.8±29.4 °C
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| Vapour Pressure |
0.0±5.0 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
2.39
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
37
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| Complexity |
1130
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(CC(=O)/C=C(\C)/[C@H]1CC(=O)[C@@]2([C@@]1(CC(=O)C3=C2[C@H](C[C@@H]4[C@@]3(CC[C@@H](C4(C)C)O)C)O)C)C)C(=O)O
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| InChi Key |
QECQJYAIIIIKJB-QQPHKSTLSA-N
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| InChi Code |
InChI=1S/C30H42O7/c1-15(10-17(31)11-16(2)26(36)37)18-12-23(35)30(7)25-19(32)13-21-27(3,4)22(34)8-9-28(21,5)24(25)20(33)14-29(18,30)6/h10,16,18-19,21-22,32,34H,8-9,11-14H2,1-7H3,(H,36,37)/b15-10+/t16?,18-,19+,21+,22+,28+,29-,30+/m1/s1
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| Chemical Name |
(E)-6-[(3S,5R,7S,10S,13R,14R,17R)-3,7-dihydroxy-4,4,10,13,14-pentamethyl-11,15-dioxo-2,3,5,6,7,12,16,17-octahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methyl-4-oxohept-5-enoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (194.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9431 mL | 9.7153 mL | 19.4307 mL | |
| 5 mM | 0.3886 mL | 1.9431 mL | 3.8861 mL | |
| 10 mM | 0.1943 mL | 0.9715 mL | 1.9431 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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