1. Autophagy
    Metabolic Enzyme/Protease
  2. Autophagy
    Cytochrome P450

Apigenin (Synonyms: 4',5,7-Trihydroxyflavone; Apigenine; Apigenol; C.I. Natural Yellow 1)

Cat. No.: HY-N1201 Purity: >98.0%
Handling Instructions

Apigenin is a competitive CYP2C9 inhibitor with a Ki of 2 μM.

For research use only. We do not sell to patients.
Apigenin Chemical Structure

Apigenin Chemical Structure

CAS No. : 520-36-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
10 mg USD 60 In-stock
50 mg USD 78 In-stock
100 mg USD 132 In-stock
200 mg USD 192 In-stock
500 mg USD 288 In-stock
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Other Forms of Apigenin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Apigenin is a competitive CYP2C9 inhibitor with a Ki of 2 μM.

IC50 & Target

Ki: 2 μM (CYP2C9)[1]

In Vitro

Apigenin inhibits cytochrome P450 2C9 (CYP2C9) with a Ki of 2 μM in the CYP2C9 RECO system (a purified, reconstituted enzyme system containing recombinant human CYP2C9, P450 reductase, cytochrome b5, and liposomes)[1]. Apigenin inhibits the cell proliferation. The growth inhibition rate (IR) of 20, 40, and 80 μM of Apigenin is 38%, 71%, and 99% respectively on the 7thd. after exposure to Apigenin for 24 or 48 h, the clone formation of SGC-7901 cells is suppressed in a dose- and time-dependent manner. The cloning efficiency in 80 μM is 9.8% and 5% after treatment with Apigenin for 24 and 48 h, while in the control group it is 40.4% and 43.4%[2].

In Vivo

Apigenin (API), a natural flavonoid, possesses a broad spectrum of biological properties, including antioxidative, anti-inflammatory, anticancer, and neuroprotective effects. Apigenin (125 mg/kg and 250  mg/kg) alleviates Adriamycin (ADR) (24 mg/kg)-induced myocardial injury. Apigenin inhibits serum aspartate amino transferase (AST) release. Apigenin reduces serum lactate dehydrogenase (LDH) release. Apigenin reduces serum creatine kinase (CK) contents[3].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.7004 mL 18.5021 mL 37.0041 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL
10 mM 0.3700 mL 1.8502 mL 3.7004 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

Apigenin is dissolved in DMSO and mixed with a fresh medium to achieve the desired concentration[2].

The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of human gastric cancer SGC-7901 cells are harvested with 0.2% EDTA and plated at a density of 2.5×103/well in 96-well microtiter plates. After an overnight incubation to allow cell attachment, the medium is replaced by fresh medium containing different concentrations (0, 20, 40, and 80 μM) of Apigenin. Control wells receive DMSO (0.2%). Each concentration of Apigenin is repeated in four wells. After incubation for 24 h, one plate is assayed with a microplate reader at the wavelength of 570 nm. Before the assay, MTT (5 mg/mL in PBS) is added to each well and incubated for 4 h, then MTT solution is removed from the wells by aspiration. After careful removal of the medium, 0.1 mL of DMSO is added to each well, and the plate is shaken for 15 min. The data of 7 d are fed into the computer and the growth curve is drawn. The growth inhibition rate (IR) is calculated[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Apigenin is mixed with 0.5% sodium carboxymethyl cellulose (CMC-Na) to form a suspension[3].

Mice[3]
Sixty healthy Kunming mice (26±2 g) are randomly assigned into two groups: a control group (n=15) and an ADR group (n=45). The ADR group is divided into three subgroups: ADR only without Apigenin (ADR, n=15), low-dose Apigenin (125 mg/kg/day, n=15), and high-dose Apigenin (250 mg/kg/day, n=15). All Apigenin-treated groups are treated daily via gastric gavage for seventeen days with a 125 or 250 mg/kg/day dose. ADR (3 mg/kg/day) is injected intraperitoneally into animals at an interval of 48 h (in total, eight times at a cumulative dose of 24 mg/kg). The mice in the control group receive injections of 0.9% sterile saline. On the 17th day after the first treatment, the mice are sacrificed, and blood samples are collected. A number of hearts are fixed with 2.5% glutaraldehyde fixative for electron microscopy analysis, and the others are stored at -80°C for western blot analysis.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

270.24

Formula

C₁₅H₁₀O₅

CAS No.

520-36-5

SMILES

OC1=C2C(OC(C3=CC=C(O)C=C3)=CC2=O)=CC(O)=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Apigenin
Cat. No.:
HY-N1201
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