| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| Other Sizes |
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| Targets |
Grosvenorine scavenges DPPH radicals (IC₅₀ = 12.3 ± 0.8 μM) and ABTS⁺ radicals (IC₅₀ = 9.7 ± 0.6 μM).
[1]
|
|---|---|
| ln Vitro |
Grosvenorine (10–100 μM) inhibited NO production in LPS-stimulated RAW 264.7 macrophages by 18–67% and reduced TNF-α secretion by 23–72%.
[1]
|
| Enzyme Assay |
DPPH assay: Grosvenorine (5–100 μM) mixed with DPPH ethanol solution, incubated for 30 min in dark. Absorbance measured at 517 nm.
ABTS assay: ABTS⁺ solution reacted with grosvenorine (5–100 μM) for 6 min. Absorbance measured at 734 nm. [1] |
| Cell Assay |
NO/TNF-α inhibition: RAW 264.7 cells pretreated with LPS (1 μg/mL) for 1 h, then incubated with grosvenorine (10–100 μM) for 24 h. NO measured by Griess reagent; TNF-α by ELISA.
[1]
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| Animal Protocol |
Pharmacokinetics: SD rats (n=6) received 20 mg/kg grosvenorine via oral gavage (suspended in 0.5% carboxymethyl cellulose). Blood collected at 0.08, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h. Plasma separated and stored at -80°C.
[1]
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| ADME/Pharmacokinetics |
Oral PK parameters: Cₘₐₓ = 142.6 ± 15.3 ng/mL, Tₘₐₓ = 0.25 h, t₁/₂ = 3.2 ± 0.4 h, AUC₀–∞ = 387.4 ± 32.1 ng·h/mL.
Metabolite identification: Six phase-II metabolites (glucuronides/sulfates) detected in plasma and bile. Biliary excretion: 23.5% of dose excreted as metabolites within 24 h. [1] |
| Toxicity/Toxicokinetics |
No acute toxicity observed at 100 mg/kg (single oral dose in rats).
[1]
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| References | |
| Additional Infomation |
Grosvenorine is a major flavonoid in Siraitia grosvenorii fruits with antioxidant and anti-inflammatory activities.
Metabolic stability: Rapidly metabolized in intestinal S9 fractions (t₁/₂ = 8.7 min) via glucuronidation. [1] Grosvenorine has been reported in Sedum sarmentosum with data available. |
| Molecular Formula |
C33H40O19
|
|---|---|
| Molecular Weight |
740.6593
|
| Exact Mass |
740.216
|
| CAS # |
156980-60-8
|
| PubChem CID |
101568804
|
| Appearance |
Off-white to light yellow solid
|
| Density |
1.7±0.1 g/cm3
|
| Boiling Point |
1067.8±65.0 °C at 760 mmHg
|
| Flash Point |
336.8±27.8 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.728
|
| LogP |
-0.65
|
| Hydrogen Bond Donor Count |
11
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
52
|
| Complexity |
1260
|
| Defined Atom Stereocenter Count |
15
|
| SMILES |
O([C@@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])O[H])[C@]1([H])[C@]([H])(OC2=C([H])C(=C3C(C(=C(C4C([H])=C([H])C(=C([H])C=4[H])O[H])OC3=C2[H])O[C@@]2([H])[C@]([H])([C@]([H])([C@]([H])([C@]([H])(C([H])([H])[H])O2)O[H])O[H])O[H])=O)O[H])O[C@@]([H])(C([H])([H])[H])[C@@]([H])([C@]1([H])O[H])O[H]
|
| InChi Key |
FFGGWIVHOGEVSP-NWQOLJAQSA-N
|
| InChi Code |
InChI=1S/C33H40O19/c1-10-19(37)23(41)26(44)31(46-10)51-29-22(40)18-15(36)7-14(8-16(18)49-28(29)12-3-5-13(35)6-4-12)48-33-30(25(43)20(38)11(2)47-33)52-32-27(45)24(42)21(39)17(9-34)50-32/h3-8,10-11,17,19-21,23-27,30-39,41-45H,9H2,1-2H3/t10-,11-,17+,19-,20-,21+,23+,24-,25+,26+,27+,30+,31-,32-,33-/m0/s1
|
| Chemical Name |
7-[(2S,3R,4R,5R,6S)-4,5-dihydroxy-6-methyl-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-5-hydroxy-2-(4-hydroxyphenyl)-3-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxychromen-4-one
|
| Synonyms |
Grosvenorine; 7-[(2S,3R,4R,5R,6S)-4,5-dihydroxy-6-methyl-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-5-hydroxy-2-(4-hydroxyphenyl)-3-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxychromen-4-one; 7-((2S,3R,4R,5R,6S)-4,5-dihydroxy-6-methyl-3-((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl)oxyoxan-2-yl)oxy-5-hydroxy-2-(4-hydroxyphenyl)-3-((2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl)oxychromen-4-one; 156980-60-8; Grosvenorin;
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~135.01 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.38 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 (3.38 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 (3.38 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 | 1.3501 mL | 6.7507 mL | 13.5015 mL | |
| 5 mM | 0.2700 mL | 1.3501 mL | 2.7003 mL | |
| 10 mM | 0.1350 mL | 0.6751 mL | 1.3501 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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