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SELGANTOLIMOD | SELGANTOLIMOD : Agonist of TLR8
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
TLR8
  • EC50:220 nM
Agonist
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
The broader selectivity profile of (R)-7 toward immune receptors was assessed in reporter gene assay ...

Potency
Cellular
In Vitro

TLR8

Mode of Action: Agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.0c00100

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.45 h
Systemic clearance: 1.8 L/h/Kg
Volume of Distribution at Steady-State: 1.1 L/Kg

DOI Reference: 10.1021/acs.jmedchem.0c00100

Dose: 5 mg/Kg
Route of delivery: Oral
Cmax: 517 ± 224 nM
Area Under the Curve:: 827 ± 540 nM*h
Bioavailability: 8.8 ± 5.7%

DOI Reference: 10.1021/acs.jmedchem.0c00100

Dog
Dose: 0.25 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.32 h
Systemic clearance: 1.2 L/h/Kg
Volume of Distribution at Steady-State: 1.01 L/Kg

DOI Reference: 10.1021/acs.jmedchem.0c00100

Dose: 0.5 mg/Kg
Route of delivery: Oral
Cmax: 9.7 ± 7.7 nM
Area Under the Curve:: 11.8 ± 7.3 nM*h
Bioavailability: 0.8 ± 0.5%

DOI Reference: 10.1021/acs.jmedchem.0c00100

Monkey (Cynomolgus)
Dose: 0.1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.67 h
Systemic clearance: 6.2 L/h/Kg
Volume of Distribution at Steady-State: 2.1 L/Kg

DOI Reference: 10.1021/acs.jmedchem.0c00100

Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 1.2 ± 0.5 nM
Area Under the Curve:: 4.7 ± 4.2 nM*h
Bioavailability: 0.3 ± 0.2%

DOI Reference: 10.1021/acs.jmedchem.0c00100

Woodchuck
Dose: 3 mg/kg once weekly for 8 weeks
Route of delivery: Oral
Target engagement assay: Plasma GS-9688 levels were approximately dose-proportional after a single oral dose of 0.3, 1, 3, and 10 mg/kg GS-9688.

DOI Reference: 10.1002/hep.31255

Chemical Information

Molecular Formula C14H20FN5O
SMILEs CCCC[C@](C)(CO)Nc1nc(N)nc2cc(F)cnc12
InChI 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
Molecular weight 293.17 Da
AlogP 2.0991999999999997
HBond acceptors 6
HBond donors 4
Atoms 41

Vendors

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Expert Reviews

by SERP
(on 18 Oct 2022)
Cellular Use Rating
In Model Organisms
Although there is no direct demonstration of in-cell target engagement and PD biomarkers are quite distal (cytokine and reporter gene endpoints), the lack of activity across a range of related receptors...
by SERP
(on 20 Oct 2022)
In Model Organisms
Extensive validation supports (R)-7 as a probe with excellent selectivity for TRL8 among the TRL family. Although biophysical characterization is limited, this probe has been well characterized in cells...
by SERP+
(on 14 Oct 2025)
Cellular Use Rating
In Model Organisms
The binding mechanism is still unclear as no co-crystal structure or relevant experimental assay has been released.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria