2. Immunology/Inflammation Apoptosis
  3. Toll-like Receptor (TLR) Interleukin Related TNF Receptor
  4. 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.

For research use only. We do not sell to patients.

TLR9 antagonist 1

TLR9 antagonist 1 Chemical Structure

CAS No. : 3105410-45-2

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TLR9 antagonist 1 Related Antibodies

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Description

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[1].

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.

TLR9 antagonist 1 Related Antibodies
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

TLR9 antagonist 1 (1-10 mg/kg; i.p.; single dose) significantly reduces the levels of proinflammatory cytokines induced by TLR9 agonists in C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice treated ODN 1668 (HY-150726)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

455.59

Formula

C28H33N5O
CAS No.
SMILES

N#CC1=C2N=CC=CC2=C(N3C(CN(CCCCNCC4=CC=CC=C4OC)C5)C5CC3)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TLR9 antagonist 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TLR9 antagonist 13105410-45-2Toll-like Receptor (TLR)Interleukin RelatedTNF ReceptorILTumor Necrosis Factor ReceptorTNFRC57BL/6J miceHEK293 reporter cellshTLR7human Toll-like receptor 9hTLR9hTLR5human peripheral blood mononuclear cellshTLR4hTLR8hTLR2Inhibitorinhibitorinhibit

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