1. Anti-infection
  2. HBV

Morphothiadin (Synonyms: GLS4)

Cat. No.: HY-108917 Purity: 99.59%
Handling Instructions

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

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

Morphothiadin Chemical Structure

Morphothiadin Chemical Structure

CAS No. : 1092970-12-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 793 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 228 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 708 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 1068 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
25 mg USD 2148 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 3240 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 4440 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 12 nM (HBV)[1]

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].

In Vivo

The area under the concentration-time curve from 0 to 24 h (AUC0-24) 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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
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.
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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

509.39

Formula

C₂₁H₂₂BrFN₄O₃S

CAS No.

1092970-12-1

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 60 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Morphothiadin
Cat. No.:
HY-108917
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