Obefazimod

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Chemical Structure| 1258453-75-6 同义名 : Abx464; SPL-464; BX-464
CAS号 : 1258453-75-6
货号 : A722436
分子式 : C16H10ClF3N2O
纯度 : 99%+
分子量 : 338.71
MDL号 : MFCD31657325
存储条件:

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Obefazimod effectively suppresses HIV-1 production in cells infected with PBMC and macrophages. It exhibits robust inhibitory action against all tested HIV-1 subtypes, including B, C, and recombinant forms. Obefazimod also strongly prevents the replication of viral strains that possess mutations granting resistance to various therapeutic drugs in vitro. Unlike the antiviral medication 3TC, which shows limited activity against K65R and M184V mutant strains, Obefazimod successfully inhibits both. In an effort to extend the understanding of Obefazimod's impact on HIV-1 replication in other primary cells, treatments range from 0.01 μM to 30 μM of Obefazimod, with monitoring of p24 antigen levels in culture supernatants across a span of 12 days. Obefazimod demonstrates a dose-responsive blockade of virus replication, with an IC50 value between 0.1 μM and 1 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.30mL

14.76mL

2.95mL

1.48mL

29.52mL

5.90mL

2.95mL

参考文献

[1]Steens JM, Scherrer D, et al. Safety, Pharmacokinetics and_Antiviral Activity of a Novel HIV Antiviral, ABX464, in Treatment- Naive HIV Infected Subjects: a Phase II Randomized, Controlled Study. Antimicrob Agents Chemother. 2017 May 15. pii: AAC.00545-17.

[2]Berkhout B, van der Velden YU. ABX464: a good drug candidate instead of a magic bullet. Retrovirology. 2015 Jul 28;12:64.