| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
| ln Vivo |
Mesoside A's average peak concentration and appearance time in rats treated with oral total saponins from Intolerantia were 162.08±139.87 ng/mL and 0.67 h, respectively. Hosenkoside A has a terminal half-life of 5.39±2.06h[1].
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|---|---|
| Animal Protocol |
Male Wistar rats (220 ± 20 g) were fasted for 12 hours prior to the experiment.
The rats were orally administered a suspension of total saponins of Semen Impatients, which was prepared by dissolving the extract in 0.5% methyl cellulose solution. The oral dose of the total saponins was 300 mg/kg body weight. The dose of Hosenkoside A contained within this total saponin extract was 12.4 mg/kg. Blood samples (approximately 0.20 mL) were collected from the suborbital vein into heparinized tubes at the following time points: before administration (0 hour), and 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, and 24 hours after dosing. The blood samples were immediately centrifuged, and the harvested plasma was stored at -80°C until analysis.[1] |
| ADME/Pharmacokinetics |
Following a single oral administration of total saponins from crocinolone cassia (equivalent to 12.4 mg/kg of crocinolone A) to rats, the mean maximum plasma concentration (Cmax) of crocinolone A was 130.99 ± 23.62 ng/mL. The time to peak concentration (Tmax) was 0.67 ± 0.13 hours. The elimination half-life (t1/2) was 5.39 ± 2.06 hours. The mean residence time (MRT) was 6.22 ± 1.91 hours. The area under the plasma concentration-time curve (AUC0-t) from time zero to the last measurable time point was 660.16 ± 262.52 ng·h/mL. The area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) was 1.50 ± 2.06 hours. The mean plasma concentration was 728.30 ± 258.35 ng·h/mL. The apparent clearance (CL/F) was 19.44 ± 8.69 L/h/kg. The apparent volume of distribution (Vd/F) was 162.08 ± 139.87 L/kg. The plasma concentration-time curve of Hosenkoside A showed a bimodal pattern, which may be related to drug interactions in the enterohepatic circulation or herbal extracts. [1]
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| References | |
| Additional Infomation |
Hosenkoside A has been reported in Impatiens balsamina, and relevant data have been reported. Hosenkoside A is a bacaloside saponin and one of the main active ingredients in Impatiens balsamina L. seeds. [1] In the total saponin extract of Impatiens balsamina seeds used in this study, the content of Hosenkoside A was 4.13%. [1] We established a sensitive and validated LC-MS/MS method for the determination of Hosenkoside A in rat plasma with a limit of quantitation (LLOQ) of 5 ng/mL. [1] The validation of this method included specificity, linearity, precision, accuracy, extraction recovery, matrix effect and stability assessment, and all results met the acceptable criteria. [1]
|
| Molecular Formula |
C48H82O20
|
|---|---|
| Molecular Weight |
979.152698040009
|
| Exact Mass |
978.539
|
| CAS # |
156791-82-1
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| PubChem CID |
102004530
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
1075.9±65.0 °C at 760 mmHg
|
| Flash Point |
604.5±34.3 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.626
|
| LogP |
0.07
|
| Hydrogen Bond Donor Count |
13
|
| Hydrogen Bond Acceptor Count |
20
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
68
|
| Complexity |
1700
|
| Defined Atom Stereocenter Count |
27
|
| SMILES |
C[C@@H](CO)[C@@H]1CC[C@@]2(CC[C@@]3([C@@H]([C@H]2O)CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H]([C@@]5(C)CO[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)CO)O)O)O)C)C)C)CO1
|
| InChi Key |
JUKFJOYCFLIWIA-MDQYKXRHSA-N
|
| InChi Code |
InChI=1S/C48H82O20/c1-22(16-49)24-8-13-48(21-62-24)15-14-46(4)23(40(48)61)6-7-29-44(2)11-10-30(45(3,28(44)9-12-47(29,46)5)20-63-41-37(59)34(56)31(53)25(17-50)64-41)67-43-39(36(58)33(55)27(19-52)66-43)68-42-38(60)35(57)32(54)26(18-51)65-42/h22-43,49-61H,6-21H2,1-5H3/t22-,23+,24-,25+,26+,27+,28+,29+,30-,31+,32+,33+,34-,35-,36-,37+,38+,39+,40+,41+,42-,43-,44-,45-,46+,47+,48+/m0/s1
|
| Chemical Name |
(2R,3R,4S,5S,6R)-2-[[(1R,2S,2'S,4aR,4bR,6aS,7R,8S,10aR,10bR,12aR)-2-[(2R,3R,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-7-hydroxy-2'-[(2S)-1-hydroxypropan-2-yl]-1,4a,10a,10b-tetramethylspiro[3,4,4b,5,6,6a,7,9,10,11,12,12a-dodecahydro-2H-chrysene-8,5'-oxane]-1-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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~51.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.55 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 (2.55 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 (2.55 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 | 1.0213 mL | 5.1065 mL | 10.2129 mL | |
| 5 mM | 0.2043 mL | 1.0213 mL | 2.0426 mL | |
| 10 mM | 0.1021 mL | 0.5106 mL | 1.0213 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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