| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| ln Vitro |
In the DPPH‑HPLC screening for antioxidants in Polygalae Radix extract, Sibiricose A5 (peak 1) showed a decrease in peak area after reaction with DPPH methanol solutions (2.5, 5, 25 mg/mL), indicating potential radical scavenging activity. The reduction in peak area was more pronounced with increasing DPPH concentration [2]
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| Animal Protocol |
For the intestinal absorption experiment using the everted rat gut sac model (in vitro, not in vivo efficacy):
Male SD rats (220‑260 g) were anesthetized with intraperitoneal injection of 2% phenobarbital sodium (0.4 mg/kg). The jejunum segment was isolated, flushed with ice‑cold Krebs‑Ringer (K‑R) solution, and cut into 10 cm lengths. The segments were everted with a smooth glass rod, tied at one end, and 2 mL of drug‑free K‑R solution was injected into the serosa compartment before tying the other end. The everted sac was suspended in 25 mL of test solution containing Sibiricose A5 (0.025, 0.050, or 0.075 mg/mL) in K‑R solution, maintained at 37°C, and continuously aerated with 5% CO₂ and 95% O₂. Serosal solution (1 mL) was sampled at 0.25, 0.75, 1.25, 2, 2.5, and 3 h, and 1 mL of drug‑free K‑R solution was injected to replace the volume. After sampling, intestinal segment length and width were measured, and uptake per unit area was calculated. [1] For co‑administration studies, Sibiricose A5 (0.050 mg/mL) was co‑incubated with verapamil (0.1 mmol/L), sodium caprate (1%), polygalaxanthone III (0.012 mg/mL), or total saponins of Polygalae Radix (TS, 1.58 mg/mL) in the same everted gut sac model. [1] |
| ADME/Pharmacokinetics |
Intestinal absorption parameters of Sibiricose A5 monomer in everted rat gut sac model (concentrations: 0.025, 0.050, 0.075 mg/mL):
- At 0.025 mg/mL: Ka = 0.0091 ± 0.0011 μg·cm⁻²·min⁻¹, Papp = 0.61 ± 0.07 ×10⁻⁵ cm/min, P% = 2.59 ± 0.23 - At 0.050 mg/mL: Ka = 0.031 ± 0.0012 μg·cm⁻²·min⁻¹ (P<0.01 vs low dose), Papp = 1.05 ± 0.039 ×10⁻⁵ cm/min (P<0.01), P% = 4.33 ± 0.13 (P<0.01) - At 0.075 mg/mL: Ka = 0.033 ± 0.0014 μg·cm⁻²·min⁻¹, Papp = 0.73 ± 0.032 ×10⁻⁵ cm/min (P<0.01 vs medium dose), P% = 3.16 ± 0.07 (P<0.01 vs medium dose) Accumulation increased linearly with time (r > 0.9) at all three concentrations. The absorption appeared saturable as concentration increased, suggesting active transport involvement. [1] When Sibiricose A5 (0.050 mg/mL) was co‑incubated with verapamil (0.1 mmol/L, P‑gp inhibitor), cumulative absorption per intestinal area increased ~1.41‑ to 1.50‑fold at 180 min (P<0.01). Ka increased to 0.044 ± 0.0077 μg·cm⁻²·min⁻¹, Papp increased from 1.34 ± 0.092 to 1.45 ± 0.093 ×10⁻⁵ cm/s (P<0.01). [1] When co‑incubated with sodium caprate (1%, paracellular enhancer), cumulative absorption increased ~1.87‑fold at 180 min (P<0.01). Ka increased to 0.061 ± 0.0077 μg·cm⁻²·min⁻¹ (P<0.01). [1] When co‑incubated with total saponins of Polygalae Radix (TS, 1.58 mg/mL), cumulative absorption increased 1.59‑fold at 180 min compared to monomer alone (P<0.01). Ka and Papp values were significantly higher than monomer alone, and the absorptive profile was close to that of PR extract. [1] When co‑incubated with polygalaxanthone III (0.012 mg/mL), no significant change in Sibiricose A5 absorption was observed. [1] In PR extract (containing SA5 at concentrations equivalent to 0.025, 0.050, 0.075 mg/mL), the absorption parameters of Sibiricose A5 were significantly higher than those of the monomer alone at all three concentrations (P<0.01). At 0.050 mg/mL in PRE: Ka = 0.048 ± 0.0011 μg·cm⁻²·min⁻¹, Papp = 1.61 ± 0.035 ×10⁻⁵ cm/min, P% = 6.60 ± 0.17. [1] |
| References |
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| Additional Infomation |
Sibiricose A5 is a hydroxycinnamic acid. It has been reported that Sibiricose A5 is present in Polygala tenuifolia, lily, and other organisms with relevant data.
Sibiricose A5 is a phenylpropanoid sucrose ester isolated from Polygala tenuifolia. Its chemical structure consists of a sucrose core with a feruloyl substituent (R1 = feruloyl, R2 = H). In the HPLC fingerprint of PR extract, Sibiricose A5 elutes in region A (0‑65 min, mixed region of oligosaccharide esters and xanthones). [1] The absorption mechanism of Sibiricose A5 appears to combine active transport (P‑gp substrate) with paracellular passive penetration, as evidenced by enhanced absorption with verapamil and sodium caprate. Total saponins of PR enhance its absorption likely via P‑gp inhibition, similar to verapamil. This is the first report of the P‑gp substrate‑like property of Sibiricose A5 and the P‑gp inhibitor‑like attribute of TS. [1] In the DPPH‑HPLC antioxidant screening, Sibiricose A5 (peak 1 at retention time 4.438 min) showed a decrease in peak area after DPPH reaction, indicating potential antioxidant activity. Its [M‑H]⁻ ion was m/z 517.1560 (calculated for C₂₂H₂₉O₁₄, 517.1563), and MS/MS fragments included m/z 160.0148 and 175.0401 ([ferulic acid‑H‑H₂O]⁻). [2] |
| Molecular Formula |
C22H30O14
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|---|---|
| Molecular Weight |
518.4652
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| Exact Mass |
518.163
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| CAS # |
107912-97-0
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| PubChem CID |
6326020
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
821.7±65.0 °C at 760 mmHg
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| Flash Point |
279.7±27.8 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
-1.69
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
36
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| Complexity |
750
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| Defined Atom Stereocenter Count |
9
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| SMILES |
COC1=C(C=CC(=C1)/C=C/C(=O)O[C@H]2[C@@H]([C@H](O[C@@]2(CO)O[C@@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)CO)O)O
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| InChi Key |
ZPEADZHVGOCGKH-YQTDNFGYSA-N
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| InChi Code |
InChI=1S/C22H30O14/c1-32-12-6-10(2-4-11(12)26)3-5-15(27)34-20-17(29)14(8-24)35-22(20,9-25)36-21-19(31)18(30)16(28)13(7-23)33-21/h2-6,13-14,16-21,23-26,28-31H,7-9H2,1H3/b5-3+/t13-,14-,16-,17-,18+,19-,20+,21-,22+/m1/s1
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| Chemical Name |
[(2S,3S,4R,5R)-4-hydroxy-2,5-bis(hydroxymethyl)-2-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-3-yl] (E)-3-(4-hydroxy-3-methoxyphenyl)prop-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 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 (~192.88 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.82 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 (4.82 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 (4.82 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 | 1.9288 mL | 9.6438 mL | 19.2875 mL | |
| 5 mM | 0.3858 mL | 1.9288 mL | 3.8575 mL | |
| 10 mM | 0.1929 mL | 0.9644 mL | 1.9288 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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