| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Loxoribine selectively targets Toll-like receptor 7 (TLR7). It acts as a TLR7 agonist, activating the innate immune system via the TLR7/MyD88-dependent signaling pathway. This leads to increased cytokine production and activation of immune cells. It is a guanine ribonucleotide derivative.
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| ln Vitro |
Loxoribine increases the Th-1- and Th-17-polarizing abilities of human monocyte-derived dendritic cells (DCs) and causes them to mature[2]. Up-regulation of CD80, CD83, CD40, CD54, and CCR7 indicates that loxoribine (250 μM; 48 hours) accelerates MoDC maturation[2]. Through the Toll-like receptor (TLR) 7/MyD88-dependent signaling pathway, loxoribine selectively activates innate immune system cells[1].
Loxoribine demonstrates immunostimulatory activity in vitro. It is a potent immunostimulatory compound that increases cytokine production. It activates cells of the innate immune system selectively via TLR7. These activities confirm its mechanism as a TLR7 agonist. |
| ln Vivo |
In vivo activation of murine natural killer (NK) cells is achieved by loxoribine (2 mg; scor iv)[3].
Loxoribine possesses antitumor and antiviral properties in vivo. It is an orally bioavailable TLR7 agonist. The compound activates immune responses that can combat viral infections and tumors. It has been studied for cancer immunotherapy and antiviral applications. |
| Enzyme Assay |
Non-cell-based receptor binding assays for Loxoribine use purified TLR7 protein or cells expressing TLR7. The compound is incubated with TLR7 and a labeled ligand or reporter system. Binding affinity is determined by measuring receptor activation using reporter gene assays or biochemical methods. TLR7/MyD88-dependent signaling can be assessed in cell-free systems.
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| Cell Assay |
Cellular assays for Loxoribine utilize immune cells such as dendritic cells, macrophages, or peripheral blood mononuclear cells (PBMCs) that express TLR7. Cells are treated with the compound at various concentrations, and cytokine production (e.g., IFN-α, IL-6, TNF-α) is measured by ELISA. Activation of downstream signaling pathways (e.g., NF-κB, IRF7) is assessed by reporter gene assays or Western blotting.
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| Animal Protocol |
Animal/Disease Models: 8-12 weeks male CBA/J mice[3]
Doses: 2 mg Route of Administration: subcutaneous (sc) or intravenous (iv) injection Experimental Results: activates murine natural killer (NK) cells in vivo. In vivo animal models for Loxoribine include tumor models to assess antitumor activity and viral infection models to assess antiviral efficacy. The compound is administered orally or via other routes. Antitumor activity is assessed by tumor growth inhibition and survival. Antiviral efficacy is assessed by viral load reduction and survival. Immune activation markers are measured to confirm mechanism of action. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Loxoribine include molecular weight of 339.30 g/mol and molecular formula C13H17N5O6. CAS number is 121288-39-9. The compound is orally bioavailable. Purity is ≥97%. Detailed PK parameters such as half-life are not extensively reported.
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| Toxicity/Toxicokinetics |
Loxoribine is an immunostimulatory compound with antitumor and antiviral properties. As a TLR7 agonist, it activates innate immune responses. Detailed toxicity data are not extensively reported. The compound is a research tool for immunology and cancer research. It has been studied for cancer immunotherapy.
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| References |
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| Additional Infomation |
Loxoribine is a guanine nucleotide derivative with immunostimulatory and immunomodulatory activities. Loxoribine enters the cytoplasm via facilitated diffusion across the plasma membrane and exerts its effects intracellularly, bypassing biochemical steps in the membrane signaling pathways utilized by B cells to activate antigens or anti-IgM antibodies. The drug activates Toll-like receptor 7 (TLR7), a member of the TLR family of pathogen-associated molecular pattern recognition receptors, thereby activating the innate immune system. This activation requires endosome maturation and recognition is limited to TLR7. Therefore, Loxoribine induces nonspecific proliferation and differentiation of proliferating B cells and recruits antigen-responsive B cells to differentiate into antibody-producing cells, thereby significantly enhancing the underlying immune response.
Loxoribine is also known as 7-Allyl-8-oxoguanosine. It has CAS number 121288-39-9. The compound is a guanosine analog with anti-viral and anti-tumor activities. It is an orally bioavailable and selective TLR7 agonist. It activates the innate immune system via TLR7/MyD88 signaling. It is a research compound for immunology. |
| Molecular Formula |
C13H17N5O6
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|---|---|
| Molecular Weight |
339.3
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| Exact Mass |
339.118
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| CAS # |
121288-39-9
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| PubChem CID |
135410906
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| Appearance |
White to off-white solid powder
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| Density |
1.92g/cm3
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| Boiling Point |
591.8ºC at 760mmHg
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| Melting Point |
227-230ºC(lit.)
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| Flash Point |
311.7ºC
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| Vapour Pressure |
1.81E-16mmHg at 25°C
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| Index of Refraction |
1.812
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| LogP |
-2.7
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
661
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C=CCN1C2=C(N=C(NC2=O)N)N(C1=O)[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O
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| InChi Key |
VDCRFBBZFHHYGT-IOSLPCCCSA-N
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| InChi Code |
InChI=1S/C13H17N5O6/c1-2-3-17-6-9(15-12(14)16-10(6)22)18(13(17)23)11-8(21)7(20)5(4-19)24-11/h2,5,7-8,11,19-21H,1,3-4H2,(H3,14,15,16,22)/t5-,7-,8-,11-/m1/s1
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| Chemical Name |
2-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-enyl-1H-purine-6,8-dione
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| Synonyms |
Loxoribinum RWJ21757 Loxoribina RWJ-21757 Loxoribine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~294.72 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9472 mL | 14.7362 mL | 29.4724 mL | |
| 5 mM | 0.5894 mL | 2.9472 mL | 5.8945 mL | |
| 10 mM | 0.2947 mL | 1.4736 mL | 2.9472 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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