Morphothiadin 是野生型和阿德福韦耐药 HBV 复制的有效抑制剂，其 IC₅₀ 值为 12 nM。

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC 50 of 12 nM.

Solid

IC50: 12 nM (HBV)

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. has not independently confirmed the accuracy of these methods. They are for reference only. <

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 &

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.
[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.

In Vitro: DMSO : 62.5 mg/mL (122.70 mM; ultrasonic and warming and heat to 60°C)配制储备液