1. Anti-infection
  2. HIV
  3. Obefazimod

Obefazimod (Synonyms: ABX464)

目录号: HY-100870 纯度: 99.98%
产品使用指南

Obefazimod (ABX464) 是一种有效的抗 HIV 剂。Obefazimod 作用于受刺激的外周血单个核细胞 (PBMCs),抑制 HIV-1 复制,IC50 为 0.1 μM 至 0.5 μM。

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Obefazimod Chemical Structure

Obefazimod Chemical Structure

CAS No. : 1258453-75-6

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Obefazimod (ABX464) is a potent anti-HIV agent. Obefazimod inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.

IC50 & Target[1]

HIV-1

0.1-0.5 μM (IC50, in PBMCs)

体外研究
(In Vitro)

Obefazimod inhibits HIV-1 production in PBMC- and macrophages-infected cells. Obefazimod has a strong inhibitory effect for all HIV-1 subtypes tested including subtype B, C and recombinant viruses. Obefazimod also very efficiently inhibits the replication of viral strains harbouring mutations that confer resistance to different therapeutic agents in vitro. While the antiviral drug 3TC is not highly active on K65R and M184V mutant strains, both strains are inhibited by Obefazimod. To generalize the effect of Obefazimod on HIV-1 replication in other primary cells, cells are treated with between 0.01 μM up to 30 μM concentrations of Obefazimod and p24 antigen levels are monitored in culture supernatants over a 12 days period. Obefazimod efficiently blocks virus replication in a dose-dependent manner with an IC50 ranging between 0.1 μM and 1 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Humanized mice reconstituted with human lymphoid cells provide rapid, reliable, reproducible experimental systems for testing the efficacy of Obefazimod in vivo. In the initial setting, SCID mice are reconstituted with PBMCs and then infected with the HIV-1 strain JR-CSF. Mice are treated twice a day (b.i.d) for 15 days by oral gavage with 20 mg/kg of Obefazimod. Measures of viral RNA show that the oral treatment with Obefazimod is able to significantly reduce the viral load over a period of 15 days of treatment. FACS analysis of blood samples show that treatment with Obefazimod prevents depletion of CD4+ cells following infection of reconstituted mice and thereby restores the CD8+/CD4+ ratio back to that of non-infected mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

338.71

Formula

C16H10ClF3N2O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (295.24 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9524 mL 14.7619 mL 29.5238 mL
5 mM 0.5905 mL 2.9524 mL 5.9048 mL
10 mM 0.2952 mL 1.4762 mL 2.9524 mL
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.75 mg/mL (11.07 mM); Clear solution

    此方案可获得 ≥ 3.75 mg/mL (11.07 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 3.75 mg/mL (11.07 mM); Clear solution

    此方案可获得 ≥ 3.75 mg/mL (11.07 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Cell Assay
[1]

The concentration of ABX464 with minimal side effects on cell viability is determined using an MTS test. PBMCs are treated with ABX464 (2, 4, 8, 16, 31, 63, 125, and 250 μM). Cell viability is measured by MTS assay after 6 days of incubation and cytotoxicity is indicated as percentage as compared with untreated cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
SCID mice are reconstituted with fresh human PBMCs for two weeks and the reconstitution rates are estimated by human IgG titration. Reconstituted SCID mice are infected with JRCSF HIV-1 strain by intraperitoneal injection. Control group receive labrafil and 5% DMSO by gavage (n=15) and the treated group receive 20 mg/kg b.i.d of ABX464 (n=14) for 15 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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HY-100870
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