Selgantolimod (Synonyms: GS-9688)
目录号: PL01760 纯度: ≥98%
CAS No. :2004677-13-6
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中文名称
Selgantolimod
英文名称
Selgantolimod
英文别名
RM4GJT3SMQ;Selgantolimod;Selgantolimod [INN];1-Hexanol, 2-((2-amino-7-fluoropyrido(3,2-d)pyrimidin-4-yl)amino)-2-methyl-, (2R)-;(2R)-2-((2-Amino-7-fluoropyrido(3,2-d)pyrimidin-4-yl)amino)-2-methylhexan-1-ol;(2R)-2-((2-Amino-7-fluoropyrido(3,2-d)pyrimidin-4-yl)amino)-2-methyl-1-hexanol;GS-9688
Cas No.
2004677-13-6
分子式
C14H20FN5O
分子量
293.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Selgantolimod (GS-9688) 是一种口服活性,有效和选择性的 Toll 样受体 8 (TLR8) 激动剂,用于乙型肝炎病毒 (HBV) 和 HIV 感染的研究。
生物活性
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.
性状
Solid
IC50 & Target[1][2]
TLR8 HBV
体外研究(In Vitro)
Selgantolimod induces the cellular immune mediators interleukin (IL)-12 and IL-8, as well as the antiviral cytokines tumor necrosis factor-α and IFN-γ in vitro in human perpheral blood mononuclear cells.
Selgantolimod activates natural killer (NK) and mucosal associated invariant T cells, stimulates cluster of differentiation (CD)-8 T-cell proliferation, and increas IFNγ production, while lowering programmed cell death protein 1 expression by HBV-specific CD8-T cells in vitro in peripheral blood mononuclear cells.
Selgantolimod-induced cytokines reduce HBV DNA, RNA, and antigen levels in HBV-infected primary human hepatocytes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Once-weekly dosing of oral Selgantolimod induces dose-dependent increases in serum IL-12 and IL-1 receptor antagonist (IL-1RA) in cynomolgus monkeys, and leads to functional cure in the woodchuck model of chronic HBV. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Jules Levin. Efficacy and Safety of Oral TLR8 Agonist Selgantolimod in Virally Suppressed Adult Patients With Chronic Hepatitis B: a Phase 2, Randomized, Double-Blind, Placebo-Controlled, Multicenter Study. 2019 Nov 8-12.
[2]. Benjamin Ryan. Selgantolimod Shows Promise as Treatment for Hepatitis B. November 18, 2019.
[3]. Romas Geleziunas, et al. Modulators of toll-like receptors for the treatme
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (213.06 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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