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Morphothiadin HBV inhibitor

Cat.No.E0094

Morphothiadin (GLS4) is a potent inhibitor on the replication of both wild-type and adefovir-resistant Hepatitis B virus (HBV) with an IC50 of 12 nM. This compound, a nucleoside analogs that target the virus polymerase, can block the HBV replication cycle and HBV-associated chronic liver diseases.
Morphothiadin HBV inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 509.39

Quality Control

Batch: E009401 DMSO]100 mg/mL]false]Ethanol]12 mg/mL]false]Water]Insoluble]false Purity: 99.87%
99.87

Chemical Information, Storage & Stability

Molecular Weight 509.39 Formula

C21H22BrFN4O3S

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1092970-12-1 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (196.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
HBV [1]
(in the Southern blotting of analysis of replicative intermediate of HBV)
12 nM
In vitro

In vitro, Morphothiadin (GLS4) is significantly less toxic for primary human hepatocytes, and inhibits virus accumulation in the supernantant of HepAD38 cells and HBV replicative forms in the liver significantly, also strongly inhibits core gene expression.[1];

In vivo

For nude mice inoculated with HepAD38 cells, treatment with this compound shows strong and sustained suppression of virus DNA to about the same extents both during and after treatment, and reduces the levels of intracellular core antigen in the tumors.[1]

References

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