| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Selgantolimod selectively targets Toll-like receptor 8 (TLR8). It activates TLR8, which is expressed on dendritic cells and macrophages, promoting the activation of both innate and adaptive immunity. This leads to the stimulation of CD8+ T cell proliferation, increased IFNγ production, and activation of natural killer (NK) and mucosal-associated invariant T cells. It also reduces programmed cell death proteins in HBV-specific CD8+ T cells.
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| ln Vitro |
In vitro, selogentolimod stimulates human peripheral blood mononuclear cells to produce the cellular immune mediators interleukin (IL)-12 and IL-8, as well as the antiviral cytokines tumor necrosis factor-α and IFN-γ [1]. Selgantolimod reduces programmed cell death proteins in HBV-specific CD8+-T cells 1 expressed in peripheral blood mononuclear cells cultured in vitro, while activating natural killer (NK) and mucosal-associated invariant T cells, stimulating CD(CD)-8+ T cell proliferation and increasing IFNγ production [1]. In HBV-infected primary human hepatocytes, cytokines generated by selagantolimod decrease HBV DNA, RNA, and antigen levels [1].
In vitro, Selgantolimod is a potent and selective TLR8 agonist with an IL-12p40 EC50 of 220 nM, demonstrating >100-fold selectivity over TLR7 (IFN-α, EC50 >50 µM). It activates immune cells, including natural killer (NK) cells and mucosal-associated invariant T cells, and stimulates CD8+ T cell proliferation and IFNγ production. It reduces programmed cell death proteins in HBV-specific CD8+ T cells. |
| ln Vivo |
In a prairie dog model of chronic HBV, once-weekly oral Selgantolimod treatment results in a dose-dependent rise in blood IL-12 and IL-1 receptor antagonist (IL-1RA) in cynomolgus monkeys and a functional cure [1].
In vivo, Selgantolimod has shown potential in enhancing immune responses against viral infections. It aims to activate the immune system to clear HBV-infected cells and reduce viral replication. Its oral bioavailability and immune-activating properties make it a promising candidate for the treatment of chronic viral infections. |
| Enzyme Assay |
In vitro receptor binding and functional assays for Selgantolimod involve measuring its activity at TLR8. Binding affinity is assessed using radioligand binding studies or surface plasmon resonance with the TLR8 receptor. Functional activity is measured in cell-based reporter assays where the compound's ability to activate TLR8-mediated signaling, such as NF-κB activation, is quantified. Its selectivity over TLR7 is confirmed in similar assays using cells expressing TLR7.
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| Cell Assay |
In vitro cellular assays for Selgantolimod are performed using human peripheral blood mononuclear cells (PBMCs) or isolated immune cell subsets. Cells are treated with the compound, and the production of cytokines such as IFN-γ, IL-12p40, and other inflammatory mediators is measured by ELISA or multiplex assays. The compound's ability to activate specific immune cell populations and enhance their function is assessed by flow cytometry.
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| Animal Protocol |
In vivo animal studies for Selgantolimod are conducted in animal models of HBV or HIV infection. The compound is administered orally, and its effects on viral load, immune cell activation, and cytokine production are measured. Its ability to reduce viral replication and enhance immune clearance is evaluated.
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| ADME/Pharmacokinetics |
Selgantolimod is an orally bioavailable compound. Upon administration, it is rapidly absorbed, leading to dose-proportional pharmacokinetic and pharmacodynamic activity. Its PK profile supports once-daily oral dosing. Detailed PK parameters such as half-life and Cmax are available from clinical trial data.
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| Toxicity/Toxicokinetics |
Toxicological data for Selgantolimod are not detailed in publicly available sources. As an immune modulator, potential toxicities could include excessive inflammation or cytokine release syndrome. Standard preclinical safety assessments would have been conducted as part of its development.
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| References | |
| Additional Infomation |
See also: Selgantolimod (note moved to).
Selgantolimod is also known as GS-9688. It is a potent and selective TLR8 agonist. It is being developed for the treatment of chronic HBV and HIV infection. It has been evaluated in clinical trials and represents a novel immunotherapeutic approach for viral infections. |
| Molecular Formula |
C14H20FN5O
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|---|---|
| Molecular Weight |
293.339905738831
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| Exact Mass |
293.165
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| CAS # |
2004677-13-6
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| PubChem CID |
122585078
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
335
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1=CN=C2C(=C1)N=C(N)N=C2N[C@](C)(CO)CCCC
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| InChi Key |
HTCJUBZBSJQWBW-CQSZACIVSA-N
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| InChi Code |
InChI=1S/C14H20FN5O/c1-3-4-5-14(2,8-21)20-12-11-10(18-13(16)19-12)6-9(15)7-17-11/h6-7,21H,3-5,8H2,1-2H3,(H3,16,18,19,20)/t14-/m1/s1
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| Chemical Name |
(2R)-2-[(2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino]-2-methylhexan-1-ol
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| Synonyms |
GS9688 GS 9688 GS-9688
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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 : ~62.5 mg/mL (~213.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.52 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 (8.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4090 mL | 17.0451 mL | 34.0901 mL | |
| 5 mM | 0.6818 mL | 3.4090 mL | 6.8180 mL | |
| 10 mM | 0.3409 mL | 1.7045 mL | 3.4090 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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