|
| | Loxoribine Basic information |
| | Loxoribine Chemical Properties |
| Melting point | 227-230 °C(lit.) | | density | 1.92±0.1 g/cm3(Predicted) | | storage temp. | Desiccate at +4°C | | solubility | Soluble in DMSO (up to 25 mg/ml). | | form | White to off-white solid. | | pka | 10.29±0.20(Predicted) | | color | White | | optical activity | [α]21/D 32°, c = 1 in H2O | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| WGK Germany | 3 | | HS Code | 29349990 |
| | Loxoribine Usage And Synthesis |
| Description | Loxoribine is a guanosine derivative and an agonist of toll-like receptor 7 (TLR7). It is selective for TLR7 over other human TLRs in a cell-based reporter assay at 1 mM.. Loxoribine induces proliferation, increases the antibody response to sheep red blood cells, and activates natural killer cell activity against Yac-1 lymphoma cells in murine splenocyte cultures (EC50s = 10-50, 3-20, and 13-22 μM, respectively). Loxoribine (250 μM) increases production of IL-12, IL-23, IL-27, and IL-10 by human monocyte-derived dendritic cells (MoDCs). Loxoribine-treated MoDCs induce higher levels of IL-17 and IFN-γ secretion by co-cultured allogeneic CD4+ T cells compared to control MoDCs. Loxoribine (120 mg/kg) reduces the number of pulmonary metastases in the B16 mouse model of melanoma, an effect enhanced by co-administration of IL-2, and exhibits adjuvant activity in mice immunized with a B16 tumor vaccine. | | Chemical Properties | White Solid | | Uses | Small-molecule immunostimulants | | Uses | Loxoribine is a selective toll-like receptor 7 (TLR7) agonist that activates immune cells and increases cytokine production. | | Uses | 7-Allyl-7,8-dihydro-8-oxoguanosine (Loxoribine) is a small-molecule immunostimulant. Loxoribine is a toll-like receptor 7 (TLR7) agonist; induces immune cell activation and increases cytokine product
ion. Loxoribine displays antitumor and antiviral activity in various animal models. | | Biological Activity | Toll-like receptor 7 (TLR7) agonist; induces immune cell activation and increases cytokine production. Displays antitumor and antiviral activity in various animal models. | | References | 1) Heil?et al.?(2003),?The Tool-like receptor 7 (TLR7)-specific stimulus loxoribine uncovers a strong relationship within the TLR7, 8 and 9 subfamily; Eur. J. Immunol.,?33?2987
2) Goodman?et al.?(1995),?A new approach to vaccine adjuvants. Immunopotentiation by intracellular T-helper-like signals transmitted by loxoribine;?Pharm. Biotechnol.,?6?581
3) Girart?et al.?(2007), Engagement of TLR3, TLR7 and NKG2D regulate IFN-gamma secretion but not NKG2D-mediated cytotoxicity by human NK cells stimulated with suboptimal doses of IL-12; J. Immunol.,?179?3472
4) Stewart?et al.?(2012),?Toll-like receptor 7 ligands inhibit influenza A infection in chickens; J. Interferon Cytokine Res,,?32?46
5) Wang?et al.?(2015),?The TLR7 agonist induces tumor regression both by promoting CD4-T cells proliferation and by reversing T regulatory cell-mediated suppression via dendritic cells; Oncotarget,?6?1779 |
| | Loxoribine Preparation Products And Raw materials |
|
