Morphothiadin (GLS4)
(Synonyms: 莫非赛定; GLS4) 目录号 : GC32073
An antiviral agent
Cas No.:1092970-12-1
Sample solution is provided at 25 µL, 10mM.
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GLS4 is an antiviral agent.1 It inhibits the replication of wild-type hepatitis B virus (HBV) and the drug-resistant HBV strains rtA181T, rtA181V, and rtN236T (IC50s = 146, 145, 161, and 131 nM, respectively). GSL4 (1 and 10 ?M) inhibits the formation of viral capsids and decreases viral core protein levels in HBV-infected HepG2 and HepG2.2.15 cells. It inhibits HBV replication and reduces the levels of viral intracellular core antigens in mice inoculated with HepAD38 cells, which carry and replicate HBV, when administered at doses ranging from 7.5 to 60 mg/kg.2
1.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 mutationsAntivir. Ther.17(5)793-803(2012) 2.Wu, G., Liu, B., Zhang, Y., et al.Preclinical characterization of GLS4, an inhibitor of hepatitis B virus core particle assemblyAntimicrob. Agents Chemother.57(11)5344-5354(2013)
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Cell experiment: |
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]. |
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Animal experiment: |
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]. |
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References: [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. |
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| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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 | 0.3926 mL | 1.9631 mL | 3.9263 mL |
| 10 mM | 0.1963 mL | 0.9816 mL | 1.9631 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet