LPRP-Et-97543 is a potent anti-HBV (hepatitis B virus) active molecule. LPRP-Et-97543 reduces Core, S, and preS activities but not X promoter activity. LPRP-Et-97543 may be utilized to study acute and chronic HBV (hepatitis B virus) infection.

Physicochemical Properties

Molecular Formula	C17H16O5
Molecular Weight	300.31
Exact Mass	300.099
CAS #	84638-48-2
PubChem CID	71585044
Appearance	Typically exists as solid at room temperature
LogP	3.2
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	2
Heavy Atom Count	22
Complexity	404
Defined Atom Stereocenter Count	1
SMILES	O=C1[C@H](CC2C=CC(O)=CC=2)COC2C=C(C(=C(C1=2)O)C)O
InChi Key	BFVOQLBTLZMHPR-LLVKDONJSA-N
InChi Code	InChI=1S/C17H16O5/c1-9-13(19)7-14-15(16(9)20)17(21)11(8-22-14)6-10-2-4-12(18)5-3-10/h2-5,7,11,18-20H,6,8H2,1H3/t11-/m1/s1
Chemical Name	(3R)-5,7-dihydroxy-3-[(4-hydroxyphenyl)methyl]-6-methyl-2,3-dihydrochromen-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
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

ln Vitro	In HepG2.2.15 and HBV-transfected Huh7 cells, LPRP-Et-97543 (0.625–40 μg/ml; 3 days) has cytotoxic effects at dosages more than 10 μg/ml[1]. The effects of LPRP-Et-97543 (2.5-10 μg/ml; 3 days) on HBsAg and HBeAg secretions are inhibitory. Furthermore, in HepG2.2.15 cells, the HBeAg inhibition rate is greater than the HBsAg inhibition rate[2]. The precore/pregenomic and major S/preS RNA are greatly reduced by LPRP-Et-97543 (2.5-10 μg/ml; 2 days after transfected with pHBV1.2 plasmid for 2 days), with the LPRP-Et-97543 inhibitory potential higher on surface RNA than on precore/pregenomic RNA[2]. In comparison to vehicle controls, LPRP-Et-97543 (2.5–10 μg/ml; 2 days after transfected with pHBV1.2 plasmid for 2 days) potently lowers intracellular levels of LHBsAg and HBcAg protein. Furthermore, in HBV-transfected Huh7 cells, LPRP-Et-97543 potently suppresses the replication of HBV DNA[2]. In Huh7 cells, LPRP-Et-97543 (2.5–10 μg/ml) decreases nuclear p65/p50 NF-κB protein expression and phosphorylated NF-κBp65 two days after transfection with pHBV1.2 plasmid[2].
Cell Assay	Western Blot Analysis[1] Cell Types: Huh7 cells with or without pHBV1.2 Tested Concentrations: 2.5-10 μg/ml Incubation Duration: 2 days Experimental Results: diminished nuclear and nuclear p-p65 expression and increased cytoplasmic IκBα expression.
References	[1]. Anti-viral effect of a compound isolated from Liriope platyphylla against hepatitis B virus in vitro.Virus Res. 2014 Nov 4;192:16-24. [2]. Naturally derived anti-hepatitis B virus agents and their mechanism of action. World J Gastroenterol. 2016 Jan 7;22(1):188-204.

Solubility Data

Solubility (In Vitro)

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

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 (e.g. IP/IV/IM/SC) 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). 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) 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). 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 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3299 mL	16.6495 mL	33.2989 mL
	5 mM	0.6660 mL	3.3299 mL	6.6598 mL
	10 mM	0.3330 mL	1.6649 mL	3.3299 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.