| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Tigloylgomisin H targets the Nrf2-ARE (Nuclear factor erythroid 2-related factor 2 - Antioxidant Response Element) signaling pathway. By activating this pathway, it upregulates the expression of phase II detoxifying enzymes, such as quinone reductase (QR). This provides a protective effect against carcinogens and oxidative stress.
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|---|---|
| ln Vitro |
In vitro, Tigloylgomisin H induces quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. It functions as a monofunctional inducer, specifically upregulating phase II enzymes through the Nrf2-ARE pathway. This activity suggests potential as a cancer chemopreventive agent.
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| ln Vivo |
In vivo, Tigloylgomisin H has potential benefits in liver cancer prevention. Its ability to upregulate phase II enzymes suggests it may protect against chemical carcinogenesis. However, specific in vivo data are limited.
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| Enzyme Assay |
In vitro non-cell enzyme assays for Tigloylgomisin H involve measuring the induction of quinone reductase (QR) activity in cell lysates. Hepa1c1c7 cells are treated with the compound, and QR activity is measured spectrophotometrically using a substrate like menadione and monitoring the reduction of a tetrazolium dye.
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| Cell Assay |
In vitro cell-based assays for Tigloylgomisin H use Hepa1c1c7 mouse hepatocarcinoma cells. Cells are treated with the compound, and the induction of QR activity is measured as described above. The activation of the Nrf2-ARE pathway can be confirmed by measuring the expression of Nrf2 target genes using qPCR or western blot.
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| Animal Protocol |
In vivo animal studies for Tigloylgomisin H would likely employ models of chemical carcinogenesis, such as the initiation-promotion model of liver cancer. The compound would be administered to the animals, and the number and size of tumors would be assessed. The induction of phase II enzymes in the liver would also be measured.
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| ADME/Pharmacokinetics |
Tigloylgomisin H has a molecular weight of 500.58 g/mol and a molecular formula of C₂₈H₃₆O₈. It has a purity of ≥98% and should be stored at 2-8°C for up to 24 months. It is a lignan with a complex structure. Detailed pharmacokinetic parameters have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of Tigloylgomisin H has not been fully characterized. As a natural compound, it is generally considered to have low toxicity. However, its potent induction of phase II enzymes suggests it could have significant biological effects that require careful evaluation.
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| References |
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| Additional Infomation |
There have been reports that Schisandra chinensis contains Gomisin H, and related data have been reported.
See also: Schisandra chinensis fruit (partial). Tigloylgomisin H is a lignan from Schisandra chinensis that induces quinone reductase activity via the Nrf2-ARE pathway. It has potential as a liver cancer prevention agent. Not approved for clinical use. |
| Molecular Formula |
C28H36O8
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|---|---|
| Molecular Weight |
500.581
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| Exact Mass |
500.241
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| CAS # |
66069-55-4
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| PubChem CID |
5318766
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
656.3±55.0 °C at 760 mmHg
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| Flash Point |
212.3±25.0 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.539
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| LogP |
4.92
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
36
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| Complexity |
771
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC=C(C)C(=O)OC1=C2C(=CC(=C1OC)OC)CC(C(CC3=CC(=C(C(=C32)OC)OC)OC)(C)O)C
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| InChi Key |
ZSAUXCVJDYCLRS-QEEHVONISA-N
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| InChi Code |
InChI=1S/C28H36O8/c1-10-15(2)27(29)36-26-21-17(12-19(31-5)24(26)34-8)11-16(3)28(4,30)14-18-13-20(32-6)23(33-7)25(35-9)22(18)21/h10,12-13,16,30H,11,14H2,1-9H3/b15-10+/t16-,28-/m0/s1
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| Chemical Name |
[(9S,10S)-10-hydroxy-4,5,14,15,16-pentamethoxy-9,10-dimethyl-3-tricyclo[10.4.0.02,7]hexadeca-1(16),2,4,6,12,14-hexaenyl] (E)-2-methylbut-2-enoate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9977 mL | 9.9884 mL | 19.9768 mL | |
| 5 mM | 0.3995 mL | 1.9977 mL | 3.9954 mL | |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9977 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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