MedChemExpress -Model Selgantolimod -2004677-13-6

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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[1][2][3].
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Selgantolimod

MCE China:Selgantolimod

Brand:MedChemExpress (MCE)

Cat. No.HY-109137

CAS:2004677-13-6

Synonyms:GS-9688

Purity:98.23%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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.

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[1]. 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[1]. Selgantolimod-induced cytokines reduce HBV DNA, RNA, and antigen levels in HBV-infected primary human hepatocytes[1].

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[1].

IC50 & Target:TLR8 HBV

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References:

[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 treatment of hiv. US20170071944A1.

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