Chrysosplenetin is one of the polymethoxylated flavonoids found in Artemisia annua and several other Chinese herbal medicines. Chrysosplenetin inhibits P-gp activity and reverses the upregulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly enhanced ART plasma levels and antimalarial efficacy in rats, in part due to its noncompetitive inhibition of rat CYP3A.

Physicochemical Properties

Molecular Formula	C19H18O8
Molecular Weight	374.3414
Exact Mass	374.1
CAS #	603-56-5
Related CAS #	603-56-5;
PubChem CID	5281608
Appearance	Light yellow to yellow solid powder
Density	1.4±0.1 g/cm3
Boiling Point	615.8±55.0 °C at 760 mmHg
Flash Point	222.7±25.0 °C
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.640
LogP	2.26
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	5
Heavy Atom Count	27
Complexity	576
Defined Atom Stereocenter Count	0
InChi Key	NBVTYGIYKCPHQN-UHFFFAOYSA-N
InChi Code	InChI=1S/C19H18O8/c1-23-11-7-9(5-6-10(11)20)17-19(26-4)16(22)14-12(27-17)8-13(24-2)18(25-3)15(14)21/h5-8,20-21H,1-4H3
Chemical Name	5-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-3,6,7-trimethoxychromen-4-one
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: 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)

Biological Activity

References	[1]. Chrysosplenetin inhibits artemisinin efflux in P-gp-over-expressing Caco-2 cells and reverses P-gp/MDR1 mRNA up-regulated expression induced by artemisinin in mouse small intestine. Pharm Biol. 2017 Dec;55(1):374-380.
Additional Infomation	Chrysosplenetin is a tetramethoxyflavone that is the 3,6,7,3'-tetramethyl ether derivative of quercetagetin. It has a role as an antiviral agent and a plant metabolite. It is a tetramethoxyflavone and a dihydroxyflavone. It is functionally related to a quercetagetin. Chrysosplenetin has been reported in Stylidocleome brachycarpa, Thulinella chrysantha, and other organisms with data available.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~267.14 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6714 mL	13.3568 mL	26.7137 mL
	5 mM	0.5343 mL	2.6714 mL	5.3427 mL
	10 mM	0.2671 mL	1.3357 mL	2.6714 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.