TLR9 antagonist 1
TLR9 antagonist 1 is a selective hTLR9 antagonist with an IC50 of 0.1 nM against hTLR9. TLR9 antagonist 1 exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 can be used in the research of systemic lupus erythematosus.
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- CAS No.: 3105410-45-2
- Formule: C28H33N5O
- Masse moléculaire:455.59
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
human TLR9 0.0001 μM (IC50) |
hTLR2 9.77 μM (IC50) |
human TLR7 2.21 μM (IC50) |
hTLR8 3.23 μM (IC50) |
hTLR4 4.75 μM (IC50) |
IL-6 |
In Vitro
TLR9 antagonist 1 (compound 38) inhibits TLR9 activity in human peripheral blood mononuclear cells with an IC50 of 4 nM[1].
TLR9 antagonist 1 exerts no significant inhibitory effect on human TLR2, TLR4 or TLR5, and exhibits a selectivity of >10000-fold for these receptors over human TLR9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUClast | F |
|---|---|---|---|---|---|---|---|
| Rat[1] | 10 (plasma) mg/kg | p.o. | 203.3 ng/mL | 7.3 h | 6.1 h | 2294.7 ng·h/mL | 30.9 % |
| Rat[1] | 10 (blood) mg/kg | p.o. | 335.6 ng/mL | 6.7 h | 6.1 h | 3437.8 ng·h/mL |
24.9 % |
| Rat[1] | 1 (plasma) mg/kg | i.v. | 269.9 ng/mL | 0.1 h | 2.9 h | 742.1 ng·h/mL | / |
| Rat[1] | 1 (blood) mg/kg | i.v. | 631.4 ng/mL | 0.1 h | 2.3 h | 1382.1 μg·h/mL | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice treated ODN 1668 (HY-150726)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly reduced serum TNF-α levels in ODN1668-challenged mice at both 3 and 6 hours post-treatment.
Potently inhibited ODN1826-induced IL-6 secretion.
Chemical Information
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CAS No. 3105410-45-2
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Masse moléculaire 455.59
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Formule C28H33N5O
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SMILES
N#CC1=C2N=CC=CC2=C(N3C(CN(CCCCNCC4=CC=CC=C4OC)C5)C5CC3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TLR9 antagonist 1 Related Classifications
HY-178037 Related Classifications
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