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Selgantolimod

Cat. No. M10713
Selgantolimod  Structure
Synonym:

GS-9688

Size Price Availability
5mg USD 540  USD540 4-7 Days
10mg USD 940  USD940 4-7 Days
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Quality Control & Documentation
Biological Activity

Selgantolimod (GS-9688) is an orally active, potent and selective Toll-like receptor 8 (TLR8) agonist for the study of hepatitis B virus (HBV) and HIV infection.

Chemical Information
Molecular Weight 293.34
Formula C14H20FN5O
CAS Number 2004677-13-6
Form Solid
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Natarajan Ayithan, et al. Viruses. Oral Selective TLR8 Agonist Selgantolimod Induces Multiple Immune Cell Responses in Humans

[2] Edward J Gane, et al. Hepatology. Safety, Pharmacokinetics, and Pharmacodynamics of the Oral TLR8 Agonist Selgantolimod in Chronic Hepatitis B

[3] Oliver E Amin, et al. Hepatology. Therapeutic Potential of TLR8 Agonist GS-9688 (Selgantolimod) in Chronic Hepatitis B: Remodeling of Antiviral and Regulatory Mediators

[4] Maribel Reyes, et al. Antivir Ther. Safety, pharmacokinetics and pharmacodynamics of selgantolimod, an oral Toll-like receptor 8 agonist: a Phase Ia study in healthy subjects

[5] Richard L Mackman, et al. J Med Chem. Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B

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