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AB-423
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AB-423图片
CAS NO:1572510-80-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 386.39
Formula C17H17F3N2O3S
CAS No. 1572510-80-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: >80 mg/mL
Water:
Ethanol:
Chemical Name
Synonyms AB 423; AB423
SMILES Code O=C(NC1=CC=C(F)C(F)=C1)C2=CC(S(=O)(N[C@H](C)CC)=O)=CC=C2F
实验参考方法
In Vitro

In vitro activity: AB-423 is a potent inhibitor of HBV capsid assembly that shows inhibitory effect on rcDNA production in AML12-HBV10 and HepDE19 cells with EC50s of ~0.260 μM. AB-423 also suppresses cccDNA formation-dependent HBeAg production in the HepBHAe82 assay with an EC50 of 0.267 μM and inhibits HBV DNA levels in culture supernatants of HepG 2.2.15 cells with an EC50 of 0.134 μM. However, AB-423 has no cytotoxicity in any of the three cell lines.


Kinase Assay:


Cell Assay: 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 leve

In VivoAB-423 (30 and 100 mg/kg, p.o. bid) inhibits 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.
Animal model NOD-SCID mice
Formulation & Dosage 30 and 100 mg/kg, p.o.
References Antimicrob Agents Chemother. 2018 May 25;62(6). pii: e00082-18.