At a concentration of 5 mg/mL, Kaempferol-7-O-β-D-glucopyranoside exhibited significant procoagulant activity in vitro using rabbit plasma. It significantly shortened the Activated Partial Thromboplastin Time (APTT), Thrombin Time (TT), and Prothrombin Time (PT) compared to the blank control group (p < 0.001). Its effect in shortening TT was significantly better than that of the positive control Yunnanbaiyao (p < 0.001). However, it also significantly decreased the Fibrinogen (FIB) content compared to the blank control (p < 0.001), although this effect was weaker than Yunnanbaiyao (p < 0.001). These results suggest its procoagulant activity may involve changes in coagulation factors in both the intrinsic and extrinsic clotting pathways.[1]
Kaempferol-7-O-β-D-glucopyranoside was identified as one of the nine major antioxidant components in Shuxuening Injection (SI) using an online ABTS⁺-CE-DAD screening method. Its antioxidant activity was demonstrated by a decrease in its peak area in the electropherogram when the SI sample was mixed online with the ABTS⁺ radical, compared to when mixed with water. This indicates its ability to scavenge the ABTS⁺ free radical. No specific quantitative potency data (e.g., IC50) for its antioxidant activity are provided.[2]
The anti-inflammatory activity of the 70% ethanol extract of Smilax bockii roots (from which Kaempferol-7-O-β-D-glucopyranoside was isolated) was evaluated. The extract showed moderate inhibitory activity against TNF-α-induced NF-κB activation in murine macrophage RAW 264.7 cells transfected with an NF-κB-mediated reporter gene construct, with an IC50 value of 166.6 µg/mL.[3]
The n-BuOH fraction (which contained Kaempferol-7-O-β-D-glucopyranoside and other flavonoids) showed relevant inhibitory activity with an IC50 value of 44.8 µg/mL, while the CHCl₃ and EtOAc fractions were nearly inactive. The study concludes that the active part inhibiting TNF-α-induced NF-κB activation was the n-BuOH fraction, but the specific contribution of Kaempferol-7-O-β-D-glucopyranoside to this activity was not tested individually.[3]

The assay for anti-inflammatory activity (inhibition of TNF-α-induced NF-κB activation) was performed using a cellular reporter gene system. Murine macrophage RAW 264.7 cells were transfected with an NF-κB-mediated reporter gene construct (presumably containing a Secreted Alkaline Phosphatase, SEAP, reporter). Cells were treated with the plant extracts (70% ethanol extract and subsequent fractions) in the presence of TNF-α to induce NF-κB activation. The inhibitory activity of the extracts on NF-κB activation was quantified, likely by measuring the SEAP activity, and reported as IC50 values. However, this assay was performed on the crude extracts and fractions, not on the isolated compound Kaempferol-7-O-β-D-glucopyranoside.[3]

[1]. Coagulatory active constituents of Malus pumila Mill. flowers. Chem Cent J. 2018 Dec 3;12(1):126.

[2]. A powerful on line ABTS+-CE-DAD method to screen and quantify major antioxidants for quality control of Shuxuening Injection. Sci Rep. 2018 Apr 3;8(1):5441.

[3]. Antiinflammatory constituents from the roots of Smilax bockii warb. Arch Pharm Res. 2005 Apr;28(4):395-9.

Kaempferol 7-O-β-D-glucopyranoside is a kaempferol O-glucopyranoside formed by the glycosidic bond between kaempferol and the β-D-glucopyranoside moiety at the 7-position. It is a metabolite, free radical scavenger, and plant metabolite. It is a β-D-glucopyranoside, kaempferol O-glucopyranoside, a monosaccharide derivative, a trihydroxyflavon, and a member of the flavonol family. Functionally, it is associated with β-D-glucose. Kaempferol-7-O-glucopyranoside has been reported in Spiranthes vernalis, Allium hirtifolium, and other organisms with relevant data. See also: Ginkgo (partial). This study is the first to isolate kaempferol-7-O-β-D-glucopyranoside (compound 2) from Malus species (and the flowers of M. pumila). It is a flavonoid glycoside. [1] This study suggests that compounds with procoagulant activity, such as kaempferol-7-O-β-D-glucopyranoside, may have the potential to treat a variety of cardiovascular diseases, suggesting that the flowers of Malus pumila may be a potential new source of bioactive molecules. [1] Kaempferol-7-O-β-D-glucopyranoside is a flavonoid glycoside that has been identified as one of the main antioxidant components in Shuxuening Injection (a preparation made from Ginkgo biloba extract). [2] Using the validated online ABTS⁺-CE-DAD method, this compound, along with eight other antioxidants, were screened, identified, and quantified in 20 different batches of Shuxuening Injection. [2] The concentrations of kaempferol-7-O-β-D-glucopyranoside in these 20 batches of Shuxuening Injection ranged from 7.0 to 10.3 μg/mL (mean ± standard deviation of each batch). [2]
The analytical method validation results of this compound showed good linearity in the range of 2.5–80 μg/mL (regression equation: y = 0.7537x – 0.8358, R² = 0.9998), with a limit of detection (MDL) of 0.04 μg/mL, a limit of quantitation (MQL) of 0.1 μg/mL, an average recovery of 100.7%, and a relative standard deviation (RSD) of 4.49%. [2]
The intra-day and inter-day accuracy of this compound at low, medium, and high concentration levels ranged from 97.3% to 106%, and it exhibited good stability. After storage at 4°C for 24 hours, its antioxidant activity ranged from 96.2% to 100%. [2]
The total antioxidant activity of Shuxuening injection was highly correlated with the total content of nine identified antioxidants (R² = 0.9456), including Kaempferol-7-O-β-D-glucopyranoside, indicating that these compounds can be used as a combination marker for quality control. [2]
Kaempferol-7-O-β-D-glucopyranoside (compound 2) was isolated from the n-butanol (n-BuOH) fraction of the 70% ethanol extract of Smilax glabra. Root. [3]
Based on the comparison of nuclear magnetic resonance spectroscopy data with literature values, this compound was identified as a known flavonoid glycoside (kaempferol-7-O-β-D-glucopyranoside). [3]
This compound was isolated from the root of Smilax glabra (S. bockii) for the first time, and also from a plant of the Smilax genus for the first time. [3]
This study aimed to identify anti-inflammatory components. Although the n-butanol extract containing the compound showed activity, the authors noted that further investigation is needed to determine the specific active compounds. [3]

C21H20O11

448.3769

448.1

16290-07-6

10095180

Light yellow to yellow solid powder

1.7±0.1 g/cm3

810.2±65.0 °C at 760 mmHg

269-271℃

287.0±27.8 °C

0.0±3.0 mmHg at 25°C

1.751

-0.19

7

11

4

32

719

5

C1=CC(=CC=C1C2=C(C(=O)C3=C(C=C(C=C3O2)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O)O

YPWHZCPMOQGCDQ-HMGRVEAOSA-N

InChI=1S/C21H20O11/c22-7-13-15(25)17(27)19(29)21(32-13)30-10-5-11(24)14-12(6-10)31-20(18(28)16(14)26)8-1-3-9(23)4-2-8/h1-6,13,15,17,19,21-25,27-29H,7H2/t13-,15-,17+,19-,21-/m1/s1

3,5-dihydroxy-2-(4-hydroxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one

2934.99.9001

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.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)