RO8191
(Synonyms: RO4948191) 目录号 : GC16956An IFNAR2 agonist
Cas No.:691868-88-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
EC50: 0.2 μM for anti-HCV activity
RO8191 is an IFN-α receptor 2 agonist.
Most acute hepatitis C virus (HCV) infections become chronic and some progress to liver cirrhosis or hepatocellular carcinoma, with thes tandard therapy involving an interferon (IFN)-α-based regimen.
In vitro: Previous study found that RO8191had remarkable anti-HCV activity. More importantly, RO8191 exerted its antiviral activity by directly interacting with the type I IFN receptor to drive IFN-stimulated genes (ISG) expression, which then induced the antiviral response of innate immune system. Previous researchers conducted a systematic structure activity relationship (SAR) study on RO8191, and although more than 100 analogues were synthesized, none of the analogues displayed improved anti-HCV activity, suggesting that RO8191 displayed a relative narrow window of SAR [1].
In vivo: A previous study evaluated the effects of RO8191 on IFN signaling in mice. Results showd that the antiviral genes were significantly induced in the livers of mice treated with RO8191. In addition, genes that had previously been reported to be induced by IFN-b in mouse liver were also induced in the livers of RO8191-treated mice. This study also measured inflammatory cytokine and chemokine expressions, and RO8191 did not significantly induce the expression of these genes. To evaluate the in-vivo anti-HCV activity of RO8191, RO8191 was orally administered to HCV-infected humanized liver mice, and the results showed that RO8191 was able to reduce HCV titer in vivo [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Wang H, Wang S, Cheng L, Chen L, Wang Y, Qing J, Huang S, Wang Y, Lei X, Wu Y, Ma Z, Zhang L, Tang Y. Discovery of Imidazo[1,2-α][1,8]naphthyridine Derivatives as Potential HCV Entry Inhibitor. ACS Med Chem Lett. 2015 Jul 27;6(9):977-81.
[2] Konishi H et al. An orally available, small-molecule interferon inhibits viral replication. Sci Rep. 2012;2:259.
| Cas No. | 691868-88-9 | SDF | |
| 别名 | RO4948191 | ||
| 化学名 | 8-(1,3,4-oxadiazol-2-yl)-2,4-bis(trifluoromethyl)-imidazo[1,2-a][1,8]naphthyridine | ||
| Canonical SMILES | FC(C1=CC(C(F)(F)F)=C2C(N3C(C=C2)=NC(C4=NN=CO4)=C3)=N1)(F)F | ||
| 分子式 | C14H5F6N5O | 分子量 | 373.2 |
| 溶解度 | ≤0.1mg/ml in DMSO;0.5mg/ml in dimethyl formamide | 储存条件 | Store at 2-8°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 | 2.6795 mL | 13.3976 mL | 26.7953 mL |
| 5 mM | 0.5359 mL | 2.6795 mL | 5.3591 mL |
| 10 mM | 0.268 mL | 1.3398 mL | 2.6795 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。