country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-187531

Copy Link Print Information

TLR7/8/9 antagonist-3

TLR7/8/9 antagonist-3 is an orally active antagonist of TLR7, TLR8 and TLR9, with human IC₅₀ values of 0.008 μM, 0.006 μM and 0.072 μM, respectively. TLR7/8/9 antagonist-3 blocks agonist-induced activation of hTLR7, hTLR8, hTLR9, mTLR7 and mTLR9, and reduces serum IFNα and TNFα levels. TLR7/8/9 antagonist-3 can be used in the research of autoimmune diseases.

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

CAS No.: 2403782-38-5
Formula: C₂₈H₃₃N₇O
Molecular Weight:483.61

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

TLR7/8/9 antagonist-3 Chemical Structure

CAS No.: 2403782-38-5

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

human TLR7

0.008 μM (IC₅₀)

hTLR8

0.006 μM (IC₅₀)

human TLR9

0.072 μM (IC₅₀)

TNF-α

All Toll-like Receptor (TLR) Isoforms :

All TNF Receptor Isoforms :

Parmacokinetics

Species	Dose	Route	AUC_0-last	F	T_1/2	V_ss	CL
Mice^[1]	2 mg/kg	i.v.	1007 ng·h/mL	/	8.4 h	7.6 L/kg	15 mL/min/kg
Mice^[1]	10 mg/kg	p.o.	631 ng·h/mL	62 %	/	/	/

In Vivo

TLR7/8/9 antagonist-3 (Compound 41) (1-300 mg/kg; p.o.; single administration) dose-dependently inhibits the activation of TLR7 and TLR9 pathways in mice. At an oral dose of 30 mg/kg, it almost completely abolishes the production of IFNα and TNFα induced by R848 (HY-13740), while at an oral dose of 300 mg/kg, it nearly fully suppresses the production of IFNα and TNFα induced by ODN2216 (HY-150741)^[1].

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

Animal Model:

BALB/c (female, 5-6 weeks old)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose
Result:

Suppressed R848-induced IFNα and TNFα production in a dose-dependent manner.
Reduced IFNα levels to near naive mouse levels at 30 mg/kg.
Reduced TNFα levels to near naive mouse levels at 30 mg/kg.

Animal Model:

BALB/c (female, 5-6 weeks old)^[1]
Dosage:

30 mg/kg; 100 mg/kg; 300 mg/kg
Administration:

p.o.; single dose
Result:

Suppressed ODN2216-induced IFNα and TNFα production in a dose-dependent manner.
Reduced IFNα levels to near naive mouse levels at 300 mg/kg.
Reduced TNFα levels to near naive mouse levels at 300 mg/kg.

Chemical Information

CAS No. 2403782-38-5
Molecular Weight 483.61
Formula C₂₈H₃₃N₇O
SMILES

N#CC1=C2N=CC=CC2=C(N3C[C@@H](C)O[C@@H](CN4CCN(C5=CC6=C(C=N5)CCNC6)CC4)C3)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

Handling Instructions (2659 KB)

References

[1]. Zhang Z, et al. Structure-Based Design of Potent TLR7/8/9 Triple Antagonists: Overcoming High Tissue Distribution and Reactive Metabolite Liabilities. Journal of medicinal chemistry. 2026 Jul 22.

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

TLR7/8/9 antagonist-3

All Toll-like Receptor (TLR) Isoforms

All TNF Receptor Isoforms