AB-423
目录号 : GC19014
AB-423 是一种 HBV 衣壳组装抑制剂，有效抑制 HBV 复制，在细胞中的 EC50/EC90 为 0.08-0.27 μM/0.33-1.32 μM。
Cas No.:1572510-80-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | To test the compound combinations, HepBHAe82 (50,000 cells/well) are plated in 96-well tissue-culture treated microtiter plates in DMEM/F12 medium supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin and tetracycline (1 μg/mL), and incubated in a humidified incubator at 37°C and 5% CO2 overnight. On the next day, the cells are switched to fresh medium and treated with inhibitor A and inhibitor B, at concentration range in the vicinity of their respective EC50 values. The inhibitors are either diluted in 100% DMSO (ETV, TDF and AB-423) or growth medium (ARB-1467 and ARB-1740) and the final DMSO concentration in the assay is ≤0.5%. The two inhibitors are tested both singly as well as in combinations determine their effects on inhibition of rcDNA production. The final DMSO concentration in the assay is 0.5%. The plates are incubated for 9 days in a humidified incubator at 37°C and 5% CO2. Following a 9 day-incubation, medium is removed, and cells are subjected to RNA extraction to measure the cccDNA-dependent precore mRNA level[1]. |
Animal experiment: | Mice[1]Prior to start of treatment, 10 micrograms of the plasmid pHBV1.3 is administered to NOD.CB17-Prkdcscid/J mice via hydrodynamic injection (HDI; rapid high volume injection into the tail vein; n = 6 to 8 animals per group). This plasmid carries a 1.3-fold overlength copy of a HBV genotype D genome which, when expressed, generates hepatitis B viral particles and other HBV products. AB-423 is administered via oral gavage at 30 or 100 mg/kg twice-daily for 7 consecutive days, starting on Day 0. Entecavir (ETV) at 100 ng/kg once-daily for 7 consecutive days, starting on Day 0. ARB-1467 is administered as a single intravenous bolus tail vein injection at 0.1 mg/kg on Day 0. Blood is collected on Days 0 (pre-dose), 4 and 7 for HBV biomarker analysis. Serum HBV DNA concentration in mice is measured from total extracted DNA using a quantitative PCR assay using primer/probe sequences[1]. |
References: [1]. Mani N, et al. Preclinical profile of AB-423, an inhibitor of Hepatitis B virus pgRNA encapsidation. Antimicrob Agents Chemother. 2018 Mar 19. | |
AB-423 is an inhibitor of HBV capsid assembly, and potent inhibits HBV replication with EC50/EC90 of 0.08-0.27 uM/0.33-1.32 uM in cells.
AB-423 is an inhibitor of HBV capsid assembly. AB-423 shows inhibitory effect on rcDNA production in AML12-HBV10 and HepDE19 cells with EC50s of ∼0.260 uM. AB-423 also suppresses cccDNA formation-dependent HBeAg production in the HepBHAe82 assay with an EC50 of 0.267 uM and inhibits HBV DNA levels in culture supernatants of HepG 2.2.15 cells with an EC50 of 0.134 uM. However, AB-423 has no cytotoxicity in any of the three cell lines[1].
AB-423 (30 and 100 mg/kg, p.o. bid) blocks HBV replication in a mouse model of HBV. AB-423 (100 mg/kg, p.o. bid) with entecavir (ETV, 100 ng/mg, qd, p.o.) or 0.1 mg/kg dose of ARB-1467 potently inhibits serum HBV DNA in an HDI model of HBV in immunodeficient NOD-SCID mice[1].
References:
[1]. Mani N, et al. Preclinical profile of AB-423, an inhibitor of Hepatitis B virus pgRNA encapsidation. Antimicrob Agents Chemother. 2018 Mar 19.
| Cas No. | 1572510-80-5 | SDF | |
| Canonical SMILES | O=C(NC1=CC=C(F)C(F)=C1)C2=CC(S(=O)(N[C@H](C)CC)=O)=CC=C2F | ||
| 分子式 | C17H17F3N2O3S | 分子量 | 386.39 |
| 溶解度 | DMSO : 83.3 mg/mL (215.59 mM) | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5881 mL | 12.9403 mL | 25.8806 mL |
| 5 mM | 0.5176 mL | 2.5881 mL | 5.1761 mL |
| 10 mM | 0.2588 mL | 1.294 mL | 2.5881 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。