| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Maltase inhibitor (IC₅₀ = 10 mM) [1]
Inhibitor of Epstein-Barr virus early antigen (EBV-EA) induction [1] |
|---|---|
| ln Vitro |
Siamenoside I inhibits the induction of Epstein-Barr virus early antigen (EBV-EA) by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells, implying potential cancer chemopreventive activity. [1]
Siamenoside I exhibits a maltase inhibitory effect with an IC₅₀ value of 10 mM. [1] |
| ln Vivo |
The processes of deglycosylation, hydroxylation, dehydrogenation, deoxygenation, isomerization, and glycosylation are among the metabolic processes of siamosaponin I in rats. The gut, stomach, kidney, brain, and other organs are the primary locations for siamenoside I and its metabolites [1].
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| Animal Protocol |
Sprague-Dawley rats (male, 210 ± 20 g) were divided into a test group (n=6) and a blank group (n=2). The test group was orally administered Siamenoside I at a dose of 50 mg/kg body weight (dissolved in normal saline) once daily at 9:00 for three consecutive days (days 3-5). The blank group received an equal volume of normal saline. On day 6, one hour after the final administration, blood was collected from the heart under anesthesia. Plasma was separated by centrifugation. Subsequently, organs (heart, liver, spleen, lungs, kidneys, stomach, small intestine, brain) and skeletal muscles were collected, washed with normal saline, and stored at -80°C until analysis. Urine and feces were collected over specified periods (days 1-2 for blank samples; 72 hours post-drug administration for test samples). [1]
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| ADME/Pharmacokinetics |
Metabolism: In rats, saminoside I undergoes extensive metabolism via a variety of pathways, including deglycosylation, hydroxylation, dehydrogenation, deoxygenation, isomerization, and glycosylation. A total of 86 metabolites were detected or preliminarily identified. Distribution: After oral administration, saminoside I and its metabolites were widely distributed in various organs of rats. The total abundance (based on peak area) of the parent drug and all its metabolites in each organ was ranked as follows: intestine > stomach > kidney > brain > liver > spleen > heart > lung. The parent drug and 14 metabolites were detected in brain tissue. The most widely distributed metabolite was mogroside IIIE (M9), which was found in all biological samples except muscle tissue. Excretion: Metabolites were detected in urine and feces. 83 metabolites were detected in feces containing the drug and 19 metabolites were detected in urine. Only two metabolites were detected in plasma, suggesting extensive first-pass metabolism and/or bile excretion. [1]
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| References | |
| Additional Infomation |
Siamenoside I is a cucurbitacin and a glycoside. Siamenoside I has been reported in Siraitia grosvenorii and Siraitia grosvenorii, and available data exist. Siamenoside I is a cucurbitane-type triterpenoid saponin (mogroside) isolated from Siraitia grosvenorii. It is considered the sweetest mogroside, with a relative sweetness 563 times that of 5% sucrose. It has been reported to inhibit two-stage carcinogenicity induced by DMBA and TPA in mice. Of its 86 identified metabolites, eight (mogroside IVA, IV, III, IIE, IA1, IE1, mogroside alcohol, and mogroside IIIE) have been shown to possess biological activity in the literature, such as inhibition of EBV-EA-induced or maltase activity, suggesting that these metabolites may contribute to the overall biological activity of Siamenoside I. Novel metabolic reactions of mogroside discovered in this study include deoxygenation, pentahydroxylation, and didehydrogenation. [1]
|
| Molecular Formula |
C54H92O24
|
|---|---|
| Molecular Weight |
1125.29000
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| Exact Mass |
1124.597
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| CAS # |
126105-12-2
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| PubChem CID |
71307460
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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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| Boiling Point |
1179.3±65.0 °C at 760 mmHg
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| Flash Point |
667.0±34.3 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.632
|
| LogP |
-0.77
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
24
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| Rotatable Bond Count |
17
|
| Heavy Atom Count |
78
|
| Complexity |
2030
|
| Defined Atom Stereocenter Count |
30
|
| SMILES |
C[C@H](CC[C@H](C(C)(C)O)O[C@H]1[C@@H]([C@H]([C@@H]([C@H](O1)CO[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)[C@H]4CC[C@@]5([C@@]4(C[C@H]([C@@]6([C@H]5CC=C7[C@H]6CC[C@@H](C7(C)C)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)CO)O)O)O)C)O)C)C
|
| InChi Key |
XJIPREFALCDWRQ-UYQGGQRHSA-N
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| InChi Code |
InChI=1S/C54H92O24/c1-22(23-15-16-52(6)30-12-10-24-25(54(30,8)31(58)17-53(23,52)7)11-14-32(50(24,2)3)76-47-43(68)39(64)35(60)27(19-56)73-47)9-13-33(51(4,5)70)77-49-45(78-48-44(69)40(65)36(61)28(20-57)74-48)41(66)37(62)29(75-49)21-71-46-42(67)38(63)34(59)26(18-55)72-46/h10,22-23,25-49,55-70H,9,11-21H2,1-8H3/t22-,23-,25-,26-,27-,28-,29-,30+,31-,32+,33-,34-,35-,36-,37-,38+,39+,40+,41+,42-,43-,44-,45-,46-,47+,48+,49+,52+,53-,54+/m1/s1
|
| Chemical Name |
(2R,3R,4S,5S,6R)-2-[[(2R,3S,4S,5R,6S)-3,4-dihydroxy-6-[(3R,6R)-2-hydroxy-6-[(3S,8S,9R,10R,11R,13R,14S,17R)-11-hydroxy-4,4,9,13,14-pentamethyl-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-2,3,7,8,10,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methylheptan-3-yl]oxy-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]methoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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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 (~88.87 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.22 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 (2.22 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 (2.22 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 | 0.8887 mL | 4.4433 mL | 8.8866 mL | |
| 5 mM | 0.1777 mL | 0.8887 mL | 1.7773 mL | |
| 10 mM | 0.0889 mL | 0.4443 mL | 0.8887 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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