Loxoribine Property

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.

Safety

WGK Germany 

3

HS Code 

29349990

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Loxoribine Chemical Properties,Usage,Production

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

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.

Uses

Loxoribine is a selective toll-like receptor 7 (TLR7) agonist that activates immune cells and increases cytokine production.

Uses

Small-molecule immunostimulants

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