Morphothiadin 是一种有效的抑制野生型和阿德福韦耐药 HBV 复制的抑制剂，IC50值为 12 nM。

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

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV (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)[2].

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].

1092970-12-1

C21H22BrFN4O3S

509.39

莫非赛定;GLS4

H2O:insoluble
DMSO:100 mg/mL (196.31 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years