Art. -Nr.: HY-108917

Morphothiadin

Name: Morphothiadin
Brand: MedChemExpress
SKU: HY-108917
Price: 120.00 USD
Availability: InStock
Rating: 5 (7 reviews)

(Synonyms: GLS4)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir (HY-B1826)-resistant HBV with an IC₅₀ of 12 nM.

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Reinheit: 99.79%
CAS. Nr.: 1092970-12-1
Formel: C₂₁H₂₂BrFN₄O₃S
Molecular Weight:509.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Morphothiadin Chemical Structure

CAS. Nr.: 1092970-12-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir (HY-B1826)-resistant HBV with an IC₅₀ of 12 nM.

IC₅₀ & Target

IC50: 12 nM (HBV)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	68.7 μM Compound: GLS4	Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
CCRF-CEM	CC₅₀	69 μM Compound: GLS4	Cytotoxicity against human CEM cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay Cytotoxicity against human CEM cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay	[PMID: 28094179]
HEK293	IC₅₀	0.86 μM Compound: GLS4; GLS4JHS	Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay	[PMID: 29381358]
HepaRG	CC₅₀	>30 μM Compound: GLS4	Cytotoxicity against human HepaRG cells assessed as effect on cell viability Cytotoxicity against human HepaRG cells assessed as effect on cell viability	[PMID: 33062174]
HepG2	CC₅₀	>100 μM Compound: GLS4	Cytotoxicity against human HepG2 cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay Cytotoxicity against human HepG2 cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay	[PMID: 28094179]
HepG2	CC₅₀	>100 μM Compound: GLS4	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
HepG2	CC₅₀	49.2 μM Compound: GLS4	Cytotoxicity in human HepG2 cells assessed as induction of cell killing Cytotoxicity in human HepG2 cells assessed as induction of cell killing	[PMID: 32421339]
HepG2	IC₅₀	0.012 μM Compound: 5; GLS4	Inhibition of HBV DNA replication in HepG2 cells by southern blot analysis Inhibition of HBV DNA replication in HepG2 cells by southern blot analysis	10.1039/C4MD00521J
HepG2 2.2.15	CC₅₀	>45 μM Compound: 8n	Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay	[PMID: 28082068]
HepG2 2.2.15	EC₅₀	0.0066 μM Compound: GLS4	Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis	[PMID: 32421339]
PBMC	CC₅₀	28 μM Compound: GLS4	Cytotoxicity against human PBMC assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay Cytotoxicity against human PBMC assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay	[PMID: 28094179]
PBMC	CC₅₀	28.4 μM Compound: GLS4	Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
Vero	CC₅₀	17.7 μM Compound: GLS4	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay	[PMID: 33421915]
Vero	CC₅₀	18 μM Compound: GLS4	Cytotoxicity against African green monkey Vero cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay Cytotoxicity against African green monkey Vero cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay	[PMID: 28094179]

In Vitro

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC₅₀ of 12 nM. Morphothiadin (GLS4) shows no toxicity up to 25 μM. The cytotoxic dose whereby 50% of cells die (CC₅₀) for primary hepatocytes is 115 μM for Morphothiadin (P<0.001). The CC₉₀ is 190 μM for Morphothiadin (P<0.01) in HepAD38 cells. Morphothiadin strongly inhibits virus accumulation in the supernatant of HepAD38 cells at 25 nM to 100 nM (P<0.02). Results show a concentration-dependent decrease of core protein in cells treated with Morphothiadin^[2].

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

In Vivo

The area under the concentration-time curve from 0 to 24 h (AUC_0-24) of Morphothiadin (GLS4) is 556 h ng/mL. After intravenous administration of 10 mg/kg Morphothiadin, the total plasma clearance and apparent volume distribution are 4.2 liters/h/kg and 7.38 liters/kg, respectively. The bioavailability of Morphothiadin is 25.5%. It is found that virus titers have increased 83.5-fold in mice treated with 3.75 mg/kg per day of Morphothiadin, 28.3-fold among mice treated with 7.5 mg/kg per day, but only 3- to 6-fold among mice treated with the higher doses of Morphothiadin. There is generally an inverse relationship between Morphothiadin dose and virus titer, with the greatest rebound seen in mice treated with 3.75 mg/kg per day of Morphothiadin (540-fold) and the smallest rebound in mice treated with 60 mg/kg per day (23-fold) (P<0.001). The Morphothiadin doses of >7.5 mg/kg per day significantly suppresses the virus replication cycle throughout the treatment period, while Morphothiadin doses of >15 mg/kg per day suppresses virus for up to 2 weeks after the end of treatment^[2].

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

Chemical Information

CAS. Nr. 1092970-12-1
Appearance Solid
Molecular Weight 509.39
Formel C₂₁H₂₂BrFN₄O₃S
Color Light yellow to yellow
SMILES

O=C(C1=C(CN2CCOCC2)NC(C3=NC=CS3)=NC1C4=CC=C(F)C=C4Br)OCC
Synonyms

GLS4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (7)

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Journal Impact Factor

Cell Mol Gastroenterol Hepatol

A Novel Mouse Model Harboring Hepatitis B Virus Covalently Closed Circular DNA. [Abstract]

2022;13(4):1001-1017. PMID: 34896285
Emerg Microbes Infect

Specific determination of hepatitis B e antigen by antibodies targeting precore unique epitope facilitates clinical diagnosis and drug evaluation against hepatitis B virus infection. [Abstract]

2021 Dec;10(1):37-50. PMID: 33296295
PLoS Pathog

HBV capsid assembly modulators differentially modulate the assembly of wild-type and drug-resistant core protein chimeric nucleocapsids and empty capsids. [Abstract]

2025 Aug 5;21(8):e1013391. PMID: 40763308
PLoS Pathog

Probing the spatiotemporal patterns of HBV multiplication reveals novel features of its subcellular processes. [Abstract]

2021 Aug 9;17(8):e1009838. PMID: 34370796
J Virol

Generation of HBV cccDNA using single-stranded M13 phage DNA for authentic minichromosome functionality. [Abstract]

2026 May 14:e0003526. PMID: 42132423
J Virol

Hepatitis B Virus Core Protein Is Not Required for Covalently Closed Circular DNA Transcriptional Regulation. [Abstract]

2022 Nov 9;96(21):e0136222. PMID: 36226986
Anal Methods

An automated microfluidic platform for the screening and characterization of novel hepatitis B virus capsid assembly modulators. [Abstract]

2022 Jan 6;14(2):135-146. PMID: 34918017

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (122.70 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9631 mL

9.8157 mL

19.6313 mL

5 mM

0.3926 mL

1.9631 mL

3.9263 mL

10 mM

0.1963 mL

0.9816 mL

1.9631 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 3 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3 mg/mL (5.89 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

HepAD38 cells are grown to about 80% confluence in 0.3 μg/mL of tetracycline (TET). After the removal of TET, the cells are treated with different doses of Morphothiadin (GLS4), or no drug. Cell viability is monitored by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay^[2].

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

Animal Administration^[2]

ICR mice are used to evaluate the pharmacokinetic (PK) properties of Morphothiadin (GLS4). Following oral administration of 10 mg/kg (of body weight) of Morphothiadin to male mice, the concentration of Morphothiadin in plasma is determined using liquid chromatography-tandem mass spectrometry (LC/MS/MS). For toxicity studies, ICR mice are given Morphothiadin by gavage over a 4-week period and then kept off drug for another 2 weeks. Groups consisting of 20 male plus 20 female mice are administered a vehicle (1% methyl-2-hydroxyethyl cellulose), 35.7, 118.9, or 356.6 mg/kg per day in a volume corresponding to 20 mL/kg. Ten mice per dose group are euthanized 2 weeks after the end of drug treatment. Body weight, food consumption, serum albumin levels, and adverse effects are determined^[2].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhou X, et al. Effects of ketoconazole and rifampicin on the pharmacokinetics of GLS4, a novel anti-hepatitis B virus compound, in dogs. Acta Pharmacol Sin. 2013 Nov;34(11):1420-6. [Content Brief]

[2]. Wu G, et al. Preclinical characterization of GLS4, an inhibitor of hepatitis B virus core particle assembly. Antimicrob Agents Chemother. 2013 Nov;57(11):5344-54. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9631 mL	9.8157 mL	19.6313 mL	49.0783 mL
	5 mM	0.3926 mL	1.9631 mL	3.9263 mL	9.8157 mL
	10 mM	0.1963 mL	0.9816 mL	1.9631 mL	4.9078 mL
	15 mM	0.1309 mL	0.6544 mL	1.3088 mL	3.2719 mL
	20 mM	0.0982 mL	0.4908 mL	0.9816 mL	2.4539 mL
	25 mM	0.0785 mL	0.3926 mL	0.7853 mL	1.9631 mL
	30 mM	0.0654 mL	0.3272 mL	0.6544 mL	1.6359 mL
	40 mM	0.0491 mL	0.2454 mL	0.4908 mL	1.2270 mL
	50 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9816 mL
	60 mM	0.0327 mL	0.1636 mL	0.3272 mL	0.8180 mL
	80 mM	0.0245 mL	0.1227 mL	0.2454 mL	0.6135 mL
	100 mM	0.0196 mL	0.0982 mL	0.1963 mL	0.4908 mL

Bioz

Keywords

Morphothiadin

7 Cited Publications

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Morphothiadin

AB-423

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GLP-26

Bersacapavir

JNJ-632

NVR 3-778

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BA-53038B

Vebicorvir

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Canocapavir

RG7834

Publications Citing Use of MedChemExpress (MCE) Morphothiadin

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Morphothiadin

AB-423

Entecavir

GLP-26

Bersacapavir

JNJ-632

NVR 3-778

Bay 41-4109

BA-53038B

Vebicorvir

Bay 41-4109 racemate

Canocapavir

RG7834

Publications Citing Use of MedChemExpress (MCE) Morphothiadin

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Morphothiadin Related Classifications

HY-108917 Related Classifications

Bioz