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

Name: Apigenin
Brand: MedChemExpress
SKU: HY-N1201
Rating: 5.0 (31 reviews)

Cat. No.: HY-N1201 Purity: 99.58%: FAQs
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Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

For research use only. We do not sell to patients.

Apigenin Chemical Structure

CAS No. : 520-36-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
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Based on 31 publication(s) in Google Scholar

Other Forms of Apigenin:

25 Publications Citing Use of MCE Apigenin

: Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]; The protein expression levels of cleaved PARP are detected from Curcumin and Apigenin-treated A375, A2058, and RPMI-7951 cell lysates compared to control samples using Western blotting analyses.

: Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]; A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

: Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]; A375, A2058, and RPMI-7951 cells were treated with DMSO (control), Curcumin (25 μM), or Apigenin (30 μM) for 24 h. Apigenin and Curcumin induce apoptosis in melanoma cells.

: Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]; Western analysis of PD-L1 expression in A375, A2058, and RPMI-7951 cells treated with IFN-γ, curcumin, or apigenin.

: Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]; A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

: Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. [Abstract]; A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

IC₅₀ & Target

CYP2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	101 μM Compound: 6	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 12027739]
B16-BL6	EC₅₀	31.6 μM Compound: 6	Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay	[PMID: 12027739]
BALB/3T3	IC₅₀	141.4 μM Compound: 4	Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay	[PMID: 10096863]
C2C12	IC₅₀	26.58 μg/mL Compound: 4	Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability by MTT assay	[PMID: 33412152]
C8166	CC₅₀	17.2 μg/mL Compound: 4	Cytotoxicity against human C8166 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human C8166 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24794743]
C8166	EC₅₀	4.46 μg/mL Compound: 4	Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity by measuring syncytial cell number after 3 days by inverted microscopic analysis Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity by measuring syncytial cell number after 3 days by inverted microscopic analysis	[PMID: 24794743]
H9	IC₅₀	35 μM Compound: 12	Cytotoxicity against human H9 cells after 3 days Cytotoxicity against human H9 cells after 3 days	[PMID: 8158164]
H9	EC₅₀	9 μM Compound: 12	Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay	[PMID: 8158164]
HCT-116	EC₅₀	23.8 μM Compound: Apigenin	Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26529431]
HEK293	IC₅₀	> 10 μM Compound: 24	Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay	[PMID: 30943030]
HEK293	IC₅₀	1.13 μM Compound: 7g	Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay	[PMID: 20731357]
HEK293	EC₅₀	24.9 μM Compound: 15	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay	[PMID: 24955889]
HeLa	IC₅₀	≥ 10 μM Compound: apigenin	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 19278239]
HeLa	IC₅₀	21.3 μM Compound: 8	Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay	[PMID: 29475587]
HeLa	EC₅₀	92.7 μM Compound: 6	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 12027739]
HeLa S3	IC₅₀	> 10 μM Compound: 9	Cytotoxicity against human HeLa S3 cells assessed as cell viability incubated for 48 hrs by microscopic analysis Cytotoxicity against human HeLa S3 cells assessed as cell viability incubated for 48 hrs by microscopic analysis	[PMID: 35704432]
HepG2	IC₅₀	70.18 μM Compound: Apigenin	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 26896708]
HL-60	IC₅₀	22.3 μM Compound: 8	Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay	[PMID: 29475587]
HT-1080	EC₅₀	36.6 μM Compound: 6	Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay	[PMID: 12027739]
HT-22	EC₅₀	> 100 μM Compound: 10	Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay Neuroprotective activity against glutamate-induced cell death in mouse HT-22 cells assessed as increase in cell viability after 24 hrs by EZ-Cytox assay	[PMID: 32991171]
Huh-7	CC₅₀	> 50 μM Compound: 21	Cytotoxicity against human Huh7.5.1 cells by MTT assay Cytotoxicity against human Huh7.5.1 cells by MTT assay	[PMID: 22445328]
Huh-7	EC₅₀	12 μM Compound: 21	Antiviral activity against HCV genotype 2a J399LM in Human Huh7.5.1 replicon cells assessed as suppression of viral replication after 72 hrs by luciferase reporter gene assay Antiviral activity against HCV genotype 2a J399LM in Human Huh7.5.1 replicon cells assessed as suppression of viral replication after 72 hrs by luciferase reporter gene assay	[PMID: 22445328]
Huh-7	EC₅₀	7.9 μM Compound: 21	Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay	[PMID: 22445328]
Jurkat	IC₅₀	1 μM Compound: Apigenin	Inhibition of chymotrypsin-like activity of human 26S proteasome in human Jurkat cells assessed as decrease in AMC hydrolysis using Z-Gly-Gly-Leu-AMC as substrate after 24 hrs by fluorescence based method Inhibition of chymotrypsin-like activity of human 26S proteasome in human Jurkat cells assessed as decrease in AMC hydrolysis using Z-Gly-Gly-Leu-AMC as substrate after 24 hrs by fluorescence based method	[PMID: 30776692]
Jurkat	IC₅₀	1.8 μM Compound: Apigenin	Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 hrs by fluorescence based method Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 hrs by fluorescence based method	[PMID: 30776692]
L02	IC₅₀	> 100 μM Compound: Apigenin	Cytotoxicity against human LO2 cells after 48 hrs by MTT assay Cytotoxicity against human LO2 cells after 48 hrs by MTT assay	[PMID: 26896708]
L6	IC₅₀	18.1 μg/mL Compound: 16	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue staining based fluorescence analysis Cytotoxicity against rat L6 cells after 72 hrs by alamar blue staining based fluorescence analysis	10.1039/C5MD00481K
L6	IC₅₀	21.8 μg/mL Compound: 16	Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by photometric method Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by photometric method	10.1039/C5MD00481K
MCF7	IC₅₀	1 μM Compound: Apigenin	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay	[PMID: 33257172]
MCF7	IC₅₀	5.9 μM Compound: 9	Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	CC₅₀	> 300 μM Compound: 1	Cytotoxicity against MDCK cells after 48 hrs by MTT assay Cytotoxicity against MDCK cells after 48 hrs by MTT assay	[PMID: 19729316]
MDCK	IC₅₀	3.1 μM Compound: 9	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	CC₅₀	39.59 μM Compound: 1	Cytotoxicity against MDCK cells by MTT assay Cytotoxicity against MDCK cells by MTT assay	[PMID: 18640042]
Monocyte	IC₅₀	1.2 μM Compound: apigenin	Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs	[PMID: 8882428]
Monocyte	IC₅₀	20 μM Compound: Apigenin	Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA	[PMID: 10096854]
MV4-11	GI₅₀	2.81 μM Compound: 2	Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay	[PMID: 23411073]
Neutrophil	IC₅₀	12.3 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay	[PMID: 23871908]
Neutrophil	IC₅₀	16.2 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay	[PMID: 23871908]
Neutrophil	IC₅₀	24 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay	[PMID: 23871908]
Neutrophil	IC₅₀	7.7 μM Compound: 4c	Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay	[PMID: 23871908]
Peritoneal macrophage	IC₅₀	7.7 μM Compound: 2;kp16	Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method	[PMID: 27955927]
RAW264.7	IC₅₀	13.4 μM Compound: 12	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 31747281]
RAW264.7	IC₅₀	14 μM Compound: 2;kp16	Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells measured after 16 hrs Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells measured after 16 hrs	[PMID: 27955927]
RAW264.7	IC₅₀	18.4 μM Compound: 18	Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay	[PMID: 33667099]
RAW264.7	IC₅₀	6.7 μM Compound: 8	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method	[PMID: 19778086]
RAW264.7	CC₅₀	65.1 μM Compound: 18	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33667099]
RAW264.7	IC₅₀	7.7 μM Compound: Apigenin	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 24 hrs by Griess reagent Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 24 hrs by Griess reagent	[PMID: 20363145]
RBL-2H3	IC₅₀	124 μM Compound: 5	Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge	[PMID: 14510616]
RS4-11	GI₅₀	27.9 μM Compound: 2	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay	[PMID: 23411073]
THP-1	IC₅₀	60 μM Compound: Apigenin	Cytotoxicity against human THP1 cells after 24 hrs by MTS assay Cytotoxicity against human THP1 cells after 24 hrs by MTS assay	[PMID: 19879672]

In Vitro

Apigenin (4',5,7-Trihydroxyflavone) inhibits cytochrome P450 2C9 (CYP2C9) with a K_i 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 cell proliferation. The growth inhibition rate (IR) of 20, 40, and 80 μM of Apigenin is 38%, 71%, and 99% respectively on the 7^thd. 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Apigenin (4',5,7-Trihydroxyflavone), 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

270.24

Formula

C₁₅H₁₀O₅

CAS No.

520-36-5

Appearance

Solid

Color

Light yellow to green yellow

SMILES

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

Structure Classification

Initial Source

Microorganisms

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (308.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (259 KB) HNMR (117 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34. [Content Brief]

[2]. Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4. [Content Brief]

[3]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676. [Content Brief]

Cell Assay ^[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]	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	[1]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34. [Content Brief] [2]. Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4. [Content Brief] [3]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.7004 mL	18.5021 mL	37.0041 mL	92.5104 mL
	5 mM	0.7401 mL	3.7004 mL	7.4008 mL	18.5021 mL
	10 mM	0.3700 mL	1.8502 mL	3.7004 mL	9.2510 mL
	15 mM	0.2467 mL	1.2335 mL	2.4669 mL	6.1674 mL
	20 mM	0.1850 mL	0.9251 mL	1.8502 mL	4.6255 mL
	25 mM	0.1480 mL	0.7401 mL	1.4802 mL	3.7004 mL
	30 mM	0.1233 mL	0.6167 mL	1.2335 mL	3.0837 mL
	40 mM	0.0925 mL	0.4626 mL	0.9251 mL	2.3128 mL
	50 mM	0.0740 mL	0.3700 mL	0.7401 mL	1.8502 mL
	60 mM	0.0617 mL	0.3084 mL	0.6167 mL	1.5418 mL
	80 mM	0.0463 mL	0.2313 mL	0.4626 mL	1.1564 mL
	100 mM	0.0370 mL	0.1850 mL	0.3700 mL	0.9251 mL

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Apigenin520-36-54',5,7-Trihydroxyflavone Apigenol C.I. Natural Yellow 1AutophagyCytochrome P450Endogenous MetaboliteCYPsInhibitorinhibitorinhibit

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

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