Morphothiadin (GLS4)是一种强效抗病毒剂，可抑制乙型肝炎病毒（HBV）复制，IC50值为12nM。
Cas No.:1092970-12-1
Sample solution is provided at 25 µL, 10mM.
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Morphothiadin (GLS4) is a potent antiviral agent that inhibits the Hepatitis B virus (HBV) replication with an IC50 value of 12nM [1]. Morphothiadin inhibits HBV replication by interfering with the assembly and disassembly of the viral nucleocapsid, suppresses the production of particles containing HBV pgRNA, and reduces the level of cccDNA[2]. Morphothiadin has been widely used to prevent HBV from infecting cells and to interfere with the formation of the viral core particles[3].
In vitro, Morphothiadin treatment for 48 hours significantly inhibited the viability of primary human hepatocytes and HepAD38 cells, with the CC50 values of 35μM and 26μM, respectively[4].
In vivo, Morphothiadin treatment via daily intragastric administration at a dose of 60mg/kg, and combined with ritonavir (40mg/kg; p.o.) for 7 days significantly reduced the HBV DNA levels in the serum of pAAV/HBV1.2 HDI mice and the expression of HBsAg in the liver, increased the expression of RIG-I in the liver tissue of the mice, and enhanced the IFN signaling pathway[5].
References:
[1] Zhou X, Gao Z, Meng J, et al. Effects of ketoconazole and rifampicin on the pharmacokinetics of GLS4, a novel anti-hepatitis B virus compound, in dogs[J]. Acta Pharmacologica Sinica, 2013, 34(11): 1420-1426.
[2] Zhang M, Gao Y, Kong F, et al. Efficacy and safety of GLS4 with entecavir vs entecavir alone in chronic hepatitis B patients: A multicenter clinical trial[J]. Journal of Infection, 2025, 90(3): 106446.
[3] Wang X Y, Wei Z M, Wu G Y, et al. In vitro inhibition of HBV replication by a novel compound, GLS4, and its efficacy against adefovir-dipivoxil-resistant HBV mutations[J]. Antiviral therapy, 2012, 17(5): 793-803.
[4] Wu G, Liu B, Zhang Y, et al. Preclinical characterization of GLS4, an inhibitor of hepatitis B virus core particle assembly[J]. Antimicrobial agents and chemotherapy, 2013, 57(11): 5344-5354.
[5] Zhao L, Xu S, Yao S, et al. GLS4 Induces the Interferon Signaling Pathway During Hepatitis B Virus (HBV) Infection[J]. Journal of Medical Virology, 2026, 98(1): e70777.
Morphothiadin (GLS4)是一种强效抗病毒剂，可抑制乙型肝炎病毒（HBV）复制，IC50值为12nM[1]。Morphothiadin通过干扰病毒核衣壳的组装和拆卸来抑制HBV复制，抑制含有HBV pgRNA的颗粒产生，并降低cccDNA水平[2]。Morphothiadin已被广泛用于预防HBV感染细胞以及干扰病毒核心颗粒的形成[3]。
在体外，Morphothiadin处理48小时显著抑制了原代人肝细胞和HepAD38细胞的活力，CC50值分别为35μM和26μM[4]。
在体内，每日灌胃给予60mg/kg剂量的Morphothiadin，联合口服ritonavir（40mg/kg），连续7天，显著降低了pAAV/HBV1.2 HDI小鼠血清中的HBV DNA水平及肝脏中HBsAg的表达，增加了小鼠肝组织中RIG-I的表达，并增强了干扰素信号通路[5]。
| Cell experiment [1]: | |
Cell lines | HepAD38 cells |
Preparation Method | HepAD38 cells were maintained in DMEM/F12 medium supplemented with 10% fetal bovine serum, and 0.3μg/ml tetracycline (TET). HepAD38 cells were seeded in 96-well microtiter plates (1×104 cells/well) for 24h at 37ºC and 5% CO2 and were treated with media containing different concentrations of Morphothiadin (0, 12.5, 25, 50, 100, 200μM) for 48h, and cell proliferation was measured. |
Reaction Conditions | 0, 12.5, 25, 50, 100, 200μM; 48h |
Applications | Morphothiadin treatment reduced the cell viability of HepAD38 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Male C57BL/6 mice (5-6 weeks old) were kept in temperature-controlled (21°C-25°C) and humidity-maintained (40%-70%) rooms with a 12-h light/dark cycle. Water and food were provided freely. The pAAV/HBV1.2 HDI mouse model was constructed by injecting 10μg pAAV/HBV1.2 plasmid via the tail vein. After 72h, the mice were treated with different therapies for 7 days. The first group (control group) was given daily intragastric administration of olive oil, the second group was given daily Morphothiadin (60mg/kg), the third group was given ritonavir (40mg/kg), and the fourth group was given daily ritonavir (40mg/kg) and Morphothiadin (60mg/kg). During gavage, peripheral blood was collected by retro-orbital bleed for analysis. |
Dosage form | 60mg/kg/day for 7 days; p.o. |
Applications | Morphothiadin treatment combined with ritonavir significantly reduced the HBV DNA levels in the serum of pAAV/HBV1.2 HDI mice. |
References: | |
| Cas No. | 1092970-12-1 | SDF | |
| 别名 | 莫非赛定; GLS4 | ||
| Canonical SMILES | O=C(C1=C(CN2CCOCC2)NC(C3=NC=CS3)=NC1C4=CC=C(F)C=C4Br)OCC | ||
| 分子式 | C21H22BrFN4O3S | 分子量 | 509.39 |
| 溶解度 | DMSO : 100 mg/mL (196.31 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9631 mL | 9.8157 mL | 19.6313 mL |
| 5 mM | 392.6 μL | 1.9631 mL | 3.9263 mL |
| 10 mM | 196.3 μL | 981.6 μL | 1.9631 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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