| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
α-glucosidase activity[1]
The primary targets of Kaempferol-7-O-rhamnoside include aldose reductase (AR), α-glucosidase, the PD-1/PD-L1 pathway, and the farnesoid X receptor (FXR). It is a potent inhibitor of the PD-1/PD-L1 pathway and an agonist of FXR. By inhibiting these targets, the compound may modulate various physiological processes, including glucose metabolism, immune response, and lipid homeostasis. |
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| ln Vitro |
In vitro, Kaempferol-7-O-rhamnoside exhibits μM-level inhibitory effects against HCT-116 and SMMC-7721 cancer cell lines. It is a moderate inhibitor of aldose reductase (AR) and a potent α-glucosidase activity inhibitor. At concentrations of 100-500 µM, the compound shows no significant cytotoxicity against H9c2 cardiomyocytes and can antagonize H2O2-induced cell damage.
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| ln Vivo |
In vivo, Kaempferol-7-O-rhamnoside may have potential therapeutic applications in diabetes, cancer, and other diseases. Its inhibition of α-glucosidase could help reduce postprandial blood glucose levels. Its inhibition of aldose reductase could help prevent diabetic complications. Its modulation of the PD-1/PD-L1 pathway and FXR could have implications for cancer immunotherapy and metabolic disorders. However, detailed in vivo studies are limited.
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| Enzyme Assay |
The in vitro enzyme assay for Kaempferol-7-O-rhamnoside involves measuring its inhibitory activity against aldose reductase, α-glucosidase, or other targets. For α-glucosidase, the enzyme is incubated with a chromogenic substrate, such as 4-nitrophenyl-α-D-glucopyranoside, in the presence of the compound. The release of 4-nitrophenol is measured spectrophotometrically at 400 nm. For aldose reductase, the enzyme is incubated with DL-glyceraldehyde and NADPH, and the decrease in NADPH absorbance is monitored at 340 nm. IC50 values are calculated by fitting dose-response curves to the inhibition data.
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| Cell Assay |
Cellular assays for Kaempferol-7-O-rhamnoside typically use cancer cell lines, such as HCT-116 and SMMC-7721, to assess its antiproliferative effects. Cells are treated with the compound at various concentrations, and cell viability is measured using standard assays such as MTT or CellTiter-Glo. The compound's effects on cell cycle progression, apoptosis, and signaling pathways may also be assessed. In cardiomyocytes (H9c2), the compound's cytoprotective effects against oxidative stress can be evaluated.
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| Animal Protocol |
In vivo animal studies for Kaempferol-7-O-rhamnoside would typically involve oral administration of the compound to rodent models of diabetes, cancer, or other diseases. Following treatment, blood glucose levels, tumor growth, and other disease-related endpoints would be assessed. The compound's effects on metabolic parameters, immune function, and tissue histology could be evaluated. However, specific in vivo study protocols for this compound are not detailed in the available literature.
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| ADME/Pharmacokinetics |
As a flavonoid glycoside, the pharmacokinetic properties of Kaempferol-7-O-rhamnoside would depend on its absorption, distribution, metabolism, and excretion characteristics. The compound has a molecular weight of 432.38 g/mol. It is likely to have moderate oral bioavailability, with metabolism by gut microbiota and hepatic enzymes. Detailed ADME parameters such as half-life, bioavailability, and tissue distribution are not available in the public domain. The compound is typically stored under standard laboratory conditions.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for Kaempferol-7-O-rhamnoside in the available literature. At concentrations of 100-500 µM, the compound shows no significant cytotoxicity against H9c2 cardiomyocytes. As a natural product and research chemical, it is generally considered safe at research doses. Standard safety precautions should be followed when handling the compound. Toxicity studies would be required if the compound were to be developed further for therapeutic applications.
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| References | |
| Additional Infomation |
Kaempferol-7-rhamnoside has been reported to have been found in Bupleurum chinense, Psyllid, and other organisms with available data.
Kaempferol-7-O-rhamnoside (CAS#: 20196-89-8) is a natural product discovered in Siraitia grosvenori. It is a flavonoid glycoside with a molecular formula of C21H20O10 and a molecular weight of 432.38. The compound exhibits μM-level inhibitory effects against HCT-116 and SMMC-7721 cancer cell lines. It is a moderate inhibitor of aldose reductase (AR) and a potent α-glucosidase activity inhibitor. It is also a potent inhibitor of the PD-1/PD-L1 pathway and an agonist of FXR. The compound has the potential for diabetes and cancer research. |
| Molecular Formula |
C21H20O10
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|---|---|
| Molecular Weight |
432.38
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| Exact Mass |
432.105
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| CAS # |
20196-89-8
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| PubChem CID |
25079965
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
753.2±60.0 °C at 760 mmHg
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| Melting Point |
231-234℃
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| Flash Point |
267.9±26.4 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.731
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
702
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)OC2=CC(=C3C(=C2)OC(=C(C3=O)O)C4=CC=C(C=C4)O)O)O)O)O
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| InChi Key |
HQNOUCSPWAGQND-GKLNBGJFSA-N
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| InChi Code |
InChI=1S/C21H20O10/c1-8-15(24)17(26)19(28)21(29-8)30-11-6-12(23)14-13(7-11)31-20(18(27)16(14)25)9-2-4-10(22)5-3-9/h2-8,15,17,19,21-24,26-28H,1H3/t8-,15-,17+,19+,21-/m0/s1
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| Chemical Name |
3,5-dihydroxy-2-(4-hydroxyphenyl)-7-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxychromen-4-one
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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) |
DMSO: 100 mg/mL (231.28 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3128 mL | 11.5639 mL | 23.1278 mL | |
| 5 mM | 0.4626 mL | 2.3128 mL | 4.6256 mL | |
| 10 mM | 0.2313 mL | 1.1564 mL | 2.3128 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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