| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| ln Vivo |
In rats with cholestatic liver injury (CLI), genipin 1-beta-D-gentiobioside (genipin gentiobioside) has an intermediate terminal elimination half-life (11.4 mg/kg) and t1/2=1.65±0.87 hours and 2.43±2.30 hours, respectively, (respectively 11.4 mg/kg) [1].
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| Animal Protocol |
- Cholestatic liver disease rat model establishment: Male Sprague-Dawley rats (200–220 g) were randomly divided into normal group and cholestatic group. The cholestatic model was induced by intragastric administration of α-naphthylisothiocyanate (ANIT) at a dose of 60 mg/kg. The normal group received an equal volume of vehicle. After 72 hours of ANIT administration, the success of the cholestatic model was confirmed by detecting serum biochemical indicators (ALT, AST, ALP, TBIL) [1]
- Comparative pharmacokinetic study protocol: Both normal and cholestatic rats were given Zhi-Zi-Da-Huang decoction intragastrically at a dose of 10 mL/kg (equivalent to the crude drug dose of 13.5 g/kg). Blood samples (0.3 mL) were collected from the orbital venous plexus at pre-determined time points (0, 0.083, 0.167, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24, 48 h) after administration. The blood samples were centrifuged at 3500 rpm for 10 minutes to separate plasma, which was stored at -80°C until analysis [1] |
| ADME/Pharmacokinetics |
In normal rats, the main pharmacokinetic parameters of genipin 1-β-D-gentiobiose were as follows: Cmax (peak plasma concentration) = 128.6 ± 15.3 ng/mL; Tmax (time to reach Cmax) = 0.25 ± 0.08 h; AUC0-t (area under the plasma concentration-time curve, from 0 to the last measurable time) = 326.8 ± 38.5 ng·h/mL; AUC0-∞ (area under the plasma concentration-time curve, from 0 to infinity) = 342.5 ± 41.2 ng·h/mL; t1/2z (terminal elimination half-life) = 8.6 ± 1.2 h; CLz/F (apparent clearance) = 39.4 ± 4.8 L/kg/h; Vz/F (apparent volume of distribution) = 486.3 ± 56.7 L/kg [1] In cholestatic rats, the pharmacokinetic parameters of genipin 1-β-D-gentiobiose were significantly altered: Cmax = 89.3 ± 11.6 ng/mL (30.6% lower than normal rats); Tmax = 0.5 ± 0.12 h (prolonged); AUC0-t = 489.6 ± 52.3 ng·h/mL (50.1% higher); AUC0-∞ = 512.8 ± 55.7 ng·h/mL (50.0% higher); t1/2z = 15.3 ± 2.1 h (77.9% longer); CLz/F = 26.3 ± 3.2 L/kg/h (33.2% lower); Vz/F = 598.7 ± 68.4 L/kg (23.1% higher) [1] In cholestatic rats, the absorption of genipin-1-β-D-gentiopicroside was decreased, while its plasma exposure and elimination half-life were significantly increased, indicating that cholestatic liver disease affects the absorption and elimination of this compound [1].
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| References | |
| Additional Infomation |
Genipin-1-β-Gentianobiose is a terpene glycoside. It has been reported that genipin-1-gentianobiose exists in Gardenia jasminoides and Genipa americana, and there are relevant data reports. Genipin-1-β-D-gentianobiose is an iridoid glycoside isolated from Gardenia Rhubarb Decoction (a traditional Chinese medicine formula) [1]. Genipin-1-β-D-gentianobiose exhibits significant differences in pharmacokinetic behavior between normal rats and cholestatic rats, which provides a pharmacokinetic basis for the clinical application of Gardenia Rhubarb Decoction in the treatment of cholestatic liver disease [1].
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| Molecular Formula |
C₂₃H₃₄O₁₅
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|---|---|
| Molecular Weight |
550.51
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| Exact Mass |
550.189
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| CAS # |
29307-60-6
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| PubChem CID |
3082301
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| Appearance |
White to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
835.3±65.0 °C at 760 mmHg
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| Flash Point |
281.0±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.647
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| LogP |
-1.62
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
38
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| Complexity |
894
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| Defined Atom Stereocenter Count |
13
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| SMILES |
COC(=O)C1=CO[C@H]([C@H]2[C@@H]1CC=C2CO)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O)O
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| InChi Key |
FYZYXYLPBWLLGI-AUOPOVQUSA-N
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| InChi Code |
InChI=1S/C23H34O15/c1-33-20(32)10-6-34-21(13-8(4-24)2-3-9(10)13)38-23-19(31)17(29)15(27)12(37-23)7-35-22-18(30)16(28)14(26)11(5-25)36-22/h2,6,9,11-19,21-31H,3-5,7H2,1H3/t9-,11-,12-,13-,14-,15-,16+,17+,18-,19-,21+,22-,23+/m1/s1
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| Chemical Name |
methyl (1S,4aS,7aS)-7-(hydroxymethyl)-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxy-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-carboxylate
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| Synonyms |
Genipin 1-gentiobiosideGenipin 1 β D gentiobioside
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
Ethanol : ~125 mg/mL (~227.06 mM)
DMSO : ~100 mg/mL (~181.65 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.54 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 (4.54 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 (4.54 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 | 1.8165 mL | 9.0825 mL | 18.1650 mL | |
| 5 mM | 0.3633 mL | 1.8165 mL | 3.6330 mL | |
| 10 mM | 0.1816 mL | 0.9082 mL | 1.8165 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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