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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Gentiopicrin is a novel and potent bioactive compound and is naturally occurring iridoid glycoside. Gentiopicrin is an inhibitor of P450 ( IC50 and a Ki of 61 µM and 22.8 µM for CYP2A6 ) and it shows potential activity of anti-inflammation and antioxidation.
ln Vitro |
Gentiopiroside has an IC50 of 61 µM and a Ki of 8.12 µM for CYP2A6, respectively, meaning that it inhibits P450 activity. With an IC50 of 1.6 mM, it also marginally suppresses CYP2E1 activity, but not CYP1A2 or CYP3A4 [1]. In a dose-dependent manner, gentiopiroside (12.5, 25, and 50 μM) inhibits the formation of osteoclasts induced by RANKL in mouse bone marrow macrophages (BMM), inhibits the expression of proteins related to osteoclasts, and stops nuclear factor-κB ligand (Receptor activator of RANKL), which activates JNK and NF-κB. Additionally, RANKL-induced bone resorption is inhibited by gentianopicroside (50 μM) [3].
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ln Vivo |
In mice, gentianopicroside (20, 40, and 80 mg/kg) significantly decreased the index of stomach ulcers. Additionally, gentiopicroside (20, 40, and 80 mg/kg) markedly decreased HSP-70, TNF-α, IL-6, and MDA levels while increasing GSH and SOD activity. Furthermore, gentiopicrin can restore mice's EGF and VEGF levels to normal [2].
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References |
[1]. Deng Y, et al. In vitro inhibition and induction of human liver cytochrome P450 enzymes by gentiopicroside: potent effect on CYP2A6. Drug Metab Pharmacokinet. 2013;28(4):339-44. Epub 2013 Feb 19.
[2]. Yang Y, et al. Protective effect of gentiopicroside from Gentiana macrophylla Pall. in ethanol-induced gastric mucosal injury in mice. Phytother Res. 2018 Feb;32(2):259-266. [3]. Chen F, et al. Gentiopicroside inhibits RANKL-induced osteoclastogenesis by regulating NF-κB and JNK signaling pathways. Biomed Pharmacother. 2018 Apr;100:142-146 |
Molecular Formula |
C16H20O9
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Molecular Weight |
356.32
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Exact Mass |
356.1107
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CAS # |
20831-76-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O1[C@]([H])([C@@]([H])([C@]([H])([C@@]([H])([C@@]1([H])C([H])([H])O[H])O[H])O[H])O[H])O[C@@]1([H])[C@]([H])(C([H])=C([H])[H])C2=C([H])C([H])([H])OC(C2=C([H])O1)=O
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Synonyms |
O 673 O-673 O673
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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) |
DMSO : ~250 mg/mL (~701.62 mM)
H2O : ≥ 100 mg/mL (~280.65 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.84 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 20.8 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: ≥ 2.08 mg/mL (5.84 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 20.8 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: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (280.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8065 mL | 14.0323 mL | 28.0647 mL | |
5 mM | 0.5613 mL | 2.8065 mL | 5.6129 mL | |
10 mM | 0.2806 mL | 1.4032 mL | 2.8065 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.