| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Targets |
iNOS; COX-2; NF-κB
Hederagenin targets multiple pathways involved in inflammation and cancer. It inhibits the expression of iNOS, COX-2, and NF-κB in LPS-stimulated cells, reducing the production of pro-inflammatory mediators. As a selective antagonist of neuropeptide FF receptor 1 (NPFR1), it blocks NPFR1-mediated signaling. Hederagenin increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. It also inhibits mitochondrial damage in Parkinson's disease via mitophagy induction. |
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| ln Vitro |
Hederagenin could induce apoptosis of LoVo cells through the mitochondrial apoptotic pathway. Hederagenin may cause procaspase-9, procaspase-3, and proPARP cleavage in addition to the up-regulation of Bax and the down-regulation of Bcl-2, Bcl-xL, and Survivin[1]. In LPS-induced RAW264.7 cells, hederagenin inhibits the pathways of NF-B, which results in a decrease in the production of pro-inflammatory mediators (NO, PGE2, TNF-α, IL-1β, and IL-6)[2].
In vitro, hederagenin demonstrates antitumor activity against multifarious cancers. It inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB in cells. Hederagenin increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. In a comparative study, hederagenin demonstrated significantly higher caspase-3 activity than the well-known apoptosis inducer staurosporine in HeLa cervical cancer cells. The compound also exhibits anti-inflammatory and neuroprotective activities. |
| ln Vivo |
In NCI-H1299 xenograft mice, hederin alone (25 mg/kg; p.o.; 11 days) had no effect on tumor growth. When combined with cisplatin (1 mg/kg), it inhibits tumor growth in a synergistic manner [4]. In mice, hederagenin (50 mg/kg; oral; once daily for 21 days) decreases 25% ethanol-induced liver damage and has anti-inflammatory and anti-apoptotic effects [5].
In vivo, hederagenin has shown pharmacological activities in the treatment of hyperlipidemia and antilipid peroxidation. Hederagenin supplementation alleviates the pro-inflammatory and apoptotic response to alcohol in rats. The compound's anti-inflammatory and neuroprotective effects have been observed in animal models, although specific experimental details are limited in the available literature. As a triterpenoid saponin, hederagenin is orally active. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for hederagenin include NPFR1 antagonism assays. The compound's binding affinity to NPFR1 can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant NPFR1. The IC50 for inhibition of NPFR1 activation is determined from dose-response curves. The compound's ability to inhibit iNOS and COX-2 can be assessed using enzyme activity assays with purified enzymes.
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| Cell Assay |
At a density of 10,000 cells per well, LoVo cells are seeded into 96-well plates. The medium is discarded and then treated with 20 μl MTT (5 mg/ml) after having been exposed to 0.25, 0.5, 1.0, 2.0, and 4.0 M hederagenin for 24 or 48 hours. The 100 μl DMSO is added to each well after the incubation period of 4 h at 37°C in order to dissolve the formed formazan crystals. At 490 nm, absorption is discovered.
In vitro cellular assays for hederagenin are performed using macrophages (RAW 264.7) or cancer cell lines. Cells are treated with hederagenin and stimulated with LPS, and NO production is measured by Griess assay. Cytokine levels (TNF-α, IL-6) are quantified by ELISA. NF-κB activation is assessed by Western blotting for p65 nuclear translocation. Cell viability is determined by MTT assay. Apoptosis is evaluated by annexin V staining and caspase activity assays. |
| Animal Protocol |
In vivo animal experiments for hederagenin are conducted in rodent models of inflammation and alcohol-induced liver injury. Rats are administered hederagenin orally, and inflammatory markers, oxidative stress, and histopathology are assessed. The compound's anti-hyperlipidemic effects can be evaluated in models of hyperlipidemia. However, detailed protocols are not extensively documented in the available literature.
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| ADME/Pharmacokinetics |
Hederagenin has a molecular weight of 472.71 g/mol and a molecular formula of C30H48O4. It is a triterpenoid saponin with orally active properties. The compound is soluble in DMSO at 10 mM. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a natural product, hederagenin may have moderate oral bioavailability and may undergo extensive metabolism in the liver.
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| Toxicity/Toxicokinetics |
The toxicological profile of hederagenin has not been extensively characterized. As a triterpenoid saponin, the compound may have hemolytic activity at high concentrations. No significant toxicity has been reported in the available literature at therapeutic doses. However, comprehensive toxicology studies would be necessary to fully assess its safety for clinical development. The compound is generally considered safe for research use.
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| References |
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| Additional Infomation |
Hederogenin is a saponin composed of oleanolic acid (12-en-28-ol) with hydroxyl groups at positions 3 and 23 (3β stereoisomer). It is a plant metabolite. It is a pentacyclic triterpenoid, a dihydroxy monocarboxylic acid, and a saponin. Functionally, it is associated with oleanolic acid. It is the conjugate acid of hederogenin (1-). It is derived from the hydride of oleanane. Hederogenin has been reported in Rosa laevigata, Dipsacus inermis, and other organisms with relevant data. See also: Paeonia lactiflora root (part); Medicago sativa whole (part); Caulophyllum robustum root (part).
Hederagenin is a triterpenoid saponin with diverse pharmacological activities, including antitumor, anti-inflammatory, and neuroprotective effects. It is also known as hederagenol. Hederagenin is a selective antagonist of neuropeptide FF receptor 1 (NPFR1) and inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. It has been studied for its potential in treating hyperlipidemia, cancer, and inflammatory diseases. Hederagenin is a research compound and is not an approved drug. Its natural abundance makes it a candidate for phytopharmaceutical applications. |
| Molecular Formula |
C30H48O4
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| Molecular Weight |
472.71
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| Exact Mass |
472.355
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| Elemental Analysis |
C, 76.23; H, 10.24; O, 13.54
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| CAS # |
465-99-6
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| Related CAS # |
465-99-6
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| PubChem CID |
73299
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
589.4±50.0 °C at 760 mmHg
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| Melting Point |
332 - 334ºC
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| Flash Point |
324.3±26.6 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
7.41
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
34
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| Complexity |
908
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C1(C)(C)C[C@@]2([H])C3=CC[C@]4([H])[C@@]5(C)CC[C@H](O)[C@@](C)(CO)[C@]5([H])CC[C@@]4(C)[C@]3(C)CC[C@@]2(C(O)=O)CC1
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| InChi Key |
PGOYMURMZNDHNS-MYPRUECHSA-N
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| InChi Code |
InChI=1S/C30H48O4/c1-25(2)13-15-30(24(33)34)16-14-28(5)19(20(30)17-25)7-8-22-26(3)11-10-23(32)27(4,18-31)21(26)9-12-29(22,28)6/h7,20-23,31-32H,8-18H2,1-6H3,(H,33,34)/t20-,21+,22+,23-,26-,27-,28+,29+,30-/m0/s1
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| Chemical Name |
(4aS,6aR,6aS,6bR,8aR,9R,10S,12aR,14bS)-10-hydroxy-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylic acid
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| Synonyms |
Astrantiagenin E; Hederagenin; Hederagenol; NSC 24954; Caulosapogenin
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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 |
| 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: 50~94 mg/mL (105.8~198.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.29 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1155 mL | 10.5773 mL | 21.1546 mL | |
| 5 mM | 0.4231 mL | 2.1155 mL | 4.2309 mL | |
| 10 mM | 0.2115 mL | 1.0577 mL | 2.1155 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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