| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | Selgantolimod | ||||||||||||
| CAS | 2004677-13-6 | ||||||||||||
| Formula | C14H20FN5O | ||||||||||||
| Molar Mass | 293.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
Selgantolimod
CAS: 2004677-13-6 F: C14H20FN5O W: 293.34
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment
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