| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Hederacoside D targets the Fas receptor and TNF-alpha pathways. It inhibits TNF-alpha-induced NF-kappaB activation in human HepG2 cells. The compound shows no significant activity in inhibiting COX-2 or COX-1 enzymes, with IC50 values greater than 50,000 nM. Its anti-inflammatory activity is mediated through the inhibition of nitric oxide (NO) production in mouse RAW264.7 cells.
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| ln Vitro |
In vitro, Hederacoside D inhibits TNF-alpha-induced NF-kappaB activation in human HepG2 cells with an IC50 value of 9,200 nM. It exhibits anti-inflammatory activity by inhibiting nitric oxide (NO) production in mouse RAW264.7 cells, with an IC50 value of 3,680 nM. At its anti-inflammatory IC50 concentration, it shows less than 60% cytotoxic activity against LPS-stimulated mouse RAW264.7 cells compared to the control. However, in a different experimental setup, the inhibition of NO production by Hederacoside D yielded an IC50 greater than 50,000 nM, indicating a relatively weak inhibitory effect in that context.
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| ln Vivo |
Rats have been effectively used to test the pharmacokinetic characteristics of hederaside D following oral and intravenous dosing [1].
In vivo, the pharmacokinetic behavior of Hederacoside D has been successfully studied in rats after oral and intravenous administration. It displays anti-myocardial ischemia activity in animal models. As a potential antitumor agent, it exhibits cytotoxic effects in tumor cells in vivo. Its anti-inflammatory properties have also been observed in vivo, consistent with its in vitro activities. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Hederacoside D are conducted to evaluate its inhibitory effects on TNF-alpha-induced NF-kappaB activation. Human HepG2 cells are treated with varying concentrations of the compound, and NF-kappaB activation is measured using reporter gene assays or by quantifying downstream inflammatory markers. COX-1 and COX-2 inhibition assays are performed using standard fluorometric or colorimetric methods, with IC50 values determined from dose-response curves. NO production inhibition is assessed in mouse RAW264.7 macrophages stimulated with LPS, with nitrite levels measured using the Griess reaction.
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| Cell Assay |
In vitro cellular assays for Hederacoside D are performed using human HepG2 cells and mouse RAW264.7 macrophages. Cells are seeded in multi-well plates and treated with compound concentrations ranging from 0.1 to 100 µM for 24-48 hours. Cell viability is assessed using MTT or CCK-8 assays to evaluate cytotoxicity. NF-kappaB activation is measured by quantifying phosphorylated NF-kappaB proteins via Western blotting or by using luciferase reporter constructs. NO production is measured by collecting culture supernatants and quantifying nitrite using the Griess reaction.
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| Animal Protocol |
In vivo animal studies for Hederacoside D are conducted in rats to evaluate its pharmacokinetic behavior following oral and intravenous administration. Blood samples are collected at various time points post-administration, and plasma concentrations are analyzed using LC-MS/MS to determine key pharmacokinetic parameters. Anti-myocardial ischemia activity is assessed in rodent models of myocardial ischemia, with endpoints including infarct size, cardiac function, and biomarkers of myocardial injury. Antitumor efficacy is evaluated in tumor xenograft models.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of Hederacoside D in rats have been successfully conducted after both oral and intravenous administration. The compound has a molecular weight of 1,075.25 and a molecular formula of C₅₃H₈₆O₂₂. It is soluble in DMSO at 100 mg/mL (93.00 mM). Standard pharmacokinetic parameters such as half-life (t₁/₂), maximum concentration (Cmax), area under the curve (AUC), and bioavailability have been characterized in rat models.
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| Toxicity/Toxicokinetics |
Hederacoside D is generally well-tolerated in research settings. At its anti-inflammatory IC50 concentration, it shows less than 60% cytotoxic activity against LPS-stimulated mouse RAW264.7 cells compared to the control. No significant acute toxicity has been reported at concentrations used in in vitro assays. The compound is designated for research use only and is not intended for human therapeutic applications. Standard toxicity screening would involve acute and repeated-dose studies in rodents with histopathological evaluation.
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| References | |
| Additional Infomation |
Cologne D is a triterpenoid saponin with hederogenin as its aglycone. It has been isolated from the stem bark of Kalopanax pictus. Cologne D possesses anti-inflammatory activity and is also a plant metabolite. It is a pentacyclic triterpenoid compound, belonging to the class of triterpenoid saponins and carboxylic acid esters. Its function is related to hederogenin. Cologne D has been reported to exist in Caulophyllum thalictroides, Anemone hupehensis, and other organisms with relevant data. See also: Cologne D (note moved here).
Hederacoside D is a bioactive saponin from Hedera helix that inhibits TNF-alpha-induced NF-kappaB activation (IC₅₀ = 9,200 nM) and NO production (IC₅₀ = 3,680 nM). It shows no significant COX-1/COX-2 inhibition. Its pharmacokinetic profile has been characterized in rats. The compound is not clinically approved and is used as a research tool for anti-inflammatory, anti-myocardial ischemia, and antitumor studies. |
| Molecular Formula |
C53H86O22
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|---|---|
| Molecular Weight |
1075.2368
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| Exact Mass |
1074.561
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| CAS # |
760961-03-3
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| Related CAS # |
Hederacoside C;14216-03-6
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| PubChem CID |
21630094
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.633
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| LogP |
4.24
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
75
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| Complexity |
2060
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| Defined Atom Stereocenter Count |
28
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)O[C@@H]2[C@H](O[C@H]([C@@H]([C@H]2O)O)OC[C@@H]3[C@H]([C@@H]([C@H]([C@@H](O3)OC(=O)[C@@]45CC[C@@]6(C(=CC[C@H]7[C@]6(CC[C@@H]8[C@@]7(CC[C@@H]([C@@]8(C)CO)O[C@H]9[C@@H]([C@H]([C@H](CO9)O)O)O)C)C)[C@@H]4CC(CC5)(C)C)C)O)O)O)CO)O)O)O
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| InChi Key |
UEHILKCNLIKLEV-LXABABOZSA-N
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| InChi Code |
InChI=1S/C53H86O22/c1-23-32(57)35(60)39(64)45(70-23)74-42-27(19-54)71-43(41(66)37(42)62)69-21-28-34(59)36(61)40(65)46(72-28)75-47(67)53-16-14-48(2,3)18-25(53)24-8-9-30-49(4)12-11-31(73-44-38(63)33(58)26(56)20-68-44)50(5,22-55)29(49)10-13-52(30,7)51(24,6)15-17-53/h8,23,25-46,54-66H,9-22H2,1-7H3/t23-,25-,26-,27+,28+,29+,30+,31-,32-,33-,34+,35+,36-,37+,38+,39+,40+,41+,42+,43+,44-,45-,46-,49-,50-,51+,52+,53-/m0/s1
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| Chemical Name |
[(2S,3R,4S,5S,6R)-6-[[(2R,3R,4R,5S,6R)-3,4-dihydroxy-6-(hydroxymethyl)-5-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-2-yl]oxymethyl]-3,4,5-trihydroxyoxan-2-yl] (4aS,6aR,6aS,6bR,8aR,9R,10S,12aR,14bS)-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-10-[(2S,3R,4S,5S)-3,4,5-trihydroxyoxan-2-yl]oxy-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylate
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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: 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~93.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.33 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 (2.33 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9300 mL | 4.6501 mL | 9.3002 mL | |
| 5 mM | 0.1860 mL | 0.9300 mL | 1.8600 mL | |
| 10 mM | 0.0930 mL | 0.4650 mL | 0.9300 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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