| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Human aldose reductase (IC50 = 43.8 ± 0.2 μM). [2]
|
|---|---|
| ln Vitro |
Ganoderic acid C2 (1) showed high inhibitory activity against human aldose reductase. At a concentration of 100 μg/mL, it exhibited 78.3 ± 0.4% inhibition. Its IC50 value was estimated to be 43.8 ± 0.2 μM. [2]
The methyl ester derivative, methyl ganoderate C2 (6), showed much less inhibitory activity on aldose reductase (34.7 ± 1.0% inhibition at 100 μg/mL, IC50 > 187.9 μM), suggesting that the free carboxyl group of ganoderic acid C2 is essential for eliciting the inhibitory activity. [2] |
| ln Vivo |
Following oral administration to rats, ganoderic acid C2 is rapidly absorbed from the gastrointestinal tract into the body fluid, with a Tmax of 3.912 minutes. It is eliminated slowly from rat plasma. A sharp peak at the end of the plasma concentration-time profile (t = 480 min) suggested a hepatoenteral circulation in the metabolism of ganoderic acid C2. [1]
|
| Enzyme Assay |
For the aldose reductase inhibition assay, the recombinant human aldose reductase enzyme was used. The reaction mixture contained 100 mM sodium phosphate buffer (pH 6.2), 0.2 mM NADPH, 0.3 M lithium sulfate, 10 mM DL-glyceraldehyde as a substrate, and the test compound (e.g., ganoderic acid C2) in 5% DMSO. The reaction was initiated by the addition of the enzyme. The mixture was incubated at 37°C for 60 minutes, and the decrease in NADPH absorbance was measured at 340 nm using a microplate reader. Quercetin was used as a positive control. The IC50 value was determined by interpolation from concentration-inhibition curves. [2]
|
| Cell Assay |
The provided documents do not describe any cell-based assays for ganoderic acid C2.
|
| Animal Protocol |
Male rats were orally administered ganoderic acid C2 at a single dose of 20 mg/kg. Blood samples were collected into heparinized tubes at various time points post-dose and immediately centrifuged to separate the plasma. The plasma samples were stored at -20°C until analysis. A liquid-liquid extraction procedure using dichloromethane-ethyl acetate (3:1, v/v) was used to extract ganoderic acid C2 and the internal standard from the rat plasma. The pharmacokinetic parameters were calculated using 3P97 software, and the concentration-time curve fitted a two-compartment model with first-order absorption. [1]
|
| ADME/Pharmacokinetics |
The pharmacokinetic parameters of ganoderic acid C2 in rat plasma after a single oral administration of 20 mg/kg are as follows: [1]
Absorption half-life (t1/2(Ka)): 3.912 min Elimination half-life (t1/2(Ke)): 213.5607 min Time to reach maximum concentration (Tmax): 3.912 min Maximum concentration (Cmax): 145.42 ng/mL Area under the curve from zero to infinity (AUC0-∞): 56600.12 (ng/mL)·min Mean residence time (MRT0-∞): 56.8 ± 32.65 min Clearance (CL/F): 0.00078 mg/kg/min Ganoderic acid C2 is the parent drug present in rat plasma after oral administration. Ten minor phase I metabolites of ganoderic acid C2 were characterized, including hydroxylation, dehydrogenation, and oxidative metabolites. A sharp peak at the end of the plasma concentration-time profile indicated hepatoenteral circulation. [1] |
| References |
|
| Additional Infomation |
Ganoderic acid C2 is a triterpenoid compound. (2R,6R)-2-methyl-4-oxo-6-[(3S,5R,7S,10S,13R,14R,15S,17R)-3,7,15-trihydroxy-4,4,10,13,14-pentamethyl-11-oxo-1,2,3,5,6,7,12,15,16,17-decahydrocyclopenta[a]phenanthrene-17-yl]heptanoic acid has been reported in Ganoderma lucidum, and relevant data are available.
Ganoderic acid C2 is a major triterpenoid from the powder of Ganoderma lucidum and generally exists in the Ganoderma genus. Previous studies indicated it possesses potential anti-tumor bioactivity, antihistamine, anti-aging, and cytotoxic effects. It is a potent aldose reductase inhibitor that may be used for the treatment of diabetic complications. The free carboxyl group of ganoderic acid C2 is essential in eliciting the aldose reductase inhibitory activity, as its methyl ester showed much lower activity. [1][2] |
| Molecular Formula |
C30H46O7
|
|---|---|
| Molecular Weight |
518.6821
|
| Exact Mass |
518.324
|
| CAS # |
103773-62-2
|
| PubChem CID |
57396771
|
| Appearance |
White to off-white solid powder
|
| Density |
1.22±0.1 g/cm3(Predicted)
|
| Boiling Point |
690.8±55.0 °C(Predicted)
|
| Melting Point |
231-232 °C
|
| LogP |
3.923
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
37
|
| Complexity |
1030
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@H](CC(=O)C[C@@H](C)C(=O)O)[C@H]1C[C@@H]([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)O
|
| InChi Key |
RERVSJVGWKIGTJ-RQLZKMEDSA-N
|
| InChi Code |
InChI=1S/C30H46O7/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/h15-16,18-19,21-23,32,34-35H,8-14H2,1-7H3,(H,36,37)/t15-,16-,18-,19+,21+,22+,23+,28+,29-,30+/m1/s1
|
| Chemical Name |
(2R,6R)-2-methyl-4-oxo-6-[(3S,5R,7S,10S,13R,14R,15S,17R)-3,7,15-trihydroxy-4,4,10,13,14-pentamethyl-11-oxo-1,2,3,5,6,7,12,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl]heptanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~96.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.41 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 12.5 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: ≥ 1.25 mg/mL (2.41 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 12.5 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: ≥ 1.25 mg/mL (2.41 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 | 1.9280 mL | 9.6399 mL | 19.2797 mL | |
| 5 mM | 0.3856 mL | 1.9280 mL | 3.8559 mL | |
| 10 mM | 0.1928 mL | 0.9640 mL | 1.9280 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
