| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
Selgantolimod (formerly GS-9688; GS9688) is a novel, potent, selective and orally bioactive toll-like receptor 8 (TLR8) agonist with the potential for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection. The potent TLR8 agonism (IL-12p40 EC50 =220 nM) and >100-fold TLR7 selectivity (IFN-α EC50 > 50 μM) was observed in human peripheral blood mononuclear cells (PBMCs).
| 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].
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| 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].
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| References | |
| Additional Infomation |
See also: Selgantolimod (annotation moved to).
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| 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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