TLR7 Activator

ssRNA40 sodium (R-1075 sodium) is a single-stranded RNA40 derived from HIV-1. ssRNA40 sodium activates the TLR7, TLR8, TLR2, RIG-I, MDA5, MyD88, Caspase-3, IRE1α, NLRP3 inflammasome and IRF7 signaling pathways. ssRNA40 sodium alters mRNA expression in neutrophils, induces pro-inflammatory cytokines, ROS, autophagy (autophagy), pyroptosis (pyroptosis), neuronal death, neurodegeneration, aggregate formation and NK cell activation. ssRNA40 sodium activates the expression of CD62L, CD11b, CD69, MX1, OAS1, ATG7, LC3B and XBP1 in immune cell and neuronal populations. ssRNA40 sodium causes cortical neuron loss and axonal damage in mice in a TLR7-dependent manner. ssRNA40 sodium can be used in research on HIV-1 infection, neurodegeneration, COVID-19 and HIV-associated neurological disorders.

ORN 06 (sodium) s a synthetic single-stranded U-rich RNA and contains 6 repeats of the UUGU sequence motif. The GU-rich oligoribonucleotides (ORNs) are able to stimulate TLR7.

INI-4001 is a TLR7/8 agonist and vaccine adjuvant. INI-4001 regulates innate and adaptive immune responses by activating murine TLR7 and human TLR7/TLR8. INI-4001 enhances IgG and neutralizing antibody responses against Powassan virus (POWV), reduces viral loads in the brain, liver and spleen, provides complete protection against lethal POWV challenge, and skews immune responses toward a Th1 phenotype. When INI-4001 is used in combination with Al (OH)₃ and SARS-CoV-2 RBD antigen, it efficiently adsorbs to Al (OH)₃, promotes Th1 immunity and enhances SARS-CoV-2 neutralizing antibody responses. INI-4001 is applicable to research related to Powassan virus infection and COVID-19.

ORN 06 (Compound R-0006), a U-rich single-stranded RNA (containing 6 repeats of the UUG sequence motif), is a TLR7/8 agonist. ORN 06 stimulates human TLR7/8-mediated or murine TLR7-mediated immunity.

ArMan is a co-activator of DC-SIGN (CD209) and TLR7. ArMan can selectively bind to DC-SIGN, promoting receptor-mediated endocytosis of the virus-like particle (VLP) platform, thereby enhancing co-binding with TLR7. ArMan can drive dendritic cell activation, shifting the immune response from humoral immunity to type 1 cellular immunity. ArMan can be used in melanoma research.

Creatine ethyl ester (CEE) is a readily available form of creatine used in supplements. Creatine ethyl ester (CEE) upregulates TLRs (TLR2, 3, 4 and TLR7) over the short-term.