TLR Antagonists

Cat.No.	Product Name	Information	Product Use Citations
S0822	TLR4-IN-C34	TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). This compound reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.	Carbohydr Polym, 2026, 373:124618 Protein Cell, 2025, pwaf020 Mol Med Rep, 2025, 32(1)177
S9730	CU-CPT9a	CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.	Nat Commun, 2024, 15(1):5678 Journal of General Virology, 2023, 1858 J Gen Virol, 2023, 104(5)001858
S4461	CU-CPT-8m	CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.	Nat Commun, 2024, 15(1):5678
S0002	IAXO-102	IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. This compound inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. It inhibits experimental abdominal aortic aneurysm (AAA) development.
E5778	CU-CPT 4a	CU-CPT 4a (TLR3-IN-1) is a potent small molecule antagonist of TLR3 with an IC50 of 3.44 µM that also inhibits TLR3/dsRNA-mediated signaling, including TNF-α and IL-1β expression. It is a valuable tool for studying protein-RNA complexes.
E4864	Pentamidine	Pentamidine (MP-601205) is an aromatic diamidine drug, an antagonist of TLR4.It also inhibits PI3K/AKT signaling pathway and reduce the expression of MMP-2 and MMP-9. It exhibits anti- protozoal, anti-inflammatory, and anti-tumor activities and is used as an agent for treating African trypanosomiasis, antimony resistant leishmaniasis and Pneumocystis carinii pneumonia.
S0835^New	TH1020	TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist, with an IC50 value of 0.85 μM. TH1020 inhibits downstream signaling pathways activated by the TLR5/Flagellin complex. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.