| Cat.No. | Name | Information |
|---|---|---|
| M4838 | TAK-242 (Resatorvid) | Resatorvid (TAK-242) is a selective TLR4 signaling inhibitor. Resatorvid inhibited the production of NO, TNF-α and IL-6 with IC50 values of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid down-regulates the expression of MyD88 and TRIF signaling molecules downstream of TLR4. Resatorvid inhibits autophagy and plays a key role in a variety of inflammatory diseases. |
| M11408 | Hydroxychloroquine | Hydroxychloroquine is a synthetic antimalarial agent that also inhibits Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine effectively inhibited SARS-COV-2 infection. |
| M9063 | TLR2-IN-C29 | C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocked HTLR2/1 and HTLR2/6 with IC50 values of 19.7 and 37.6 μM, respectively. |
| M42066 | Polyinosinic acid | Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) agonist. |
| M5062 | Polyinosinic acid: polycytidylic acid (poly I:C) | Polyinosinic acid: polycytidylic acid (poly I:C) is a synthetic polyinosinic-polycytidylic acid double-stranded RNA. Polyinosinic-polycytidylic acid (Poly (I:C)) is an agonist of toll-like receptor (TLR)-3. Polyinosinic-polycytidylic acid has protective effects against cerebral ischemia/reperfusion (I/R) injury and can be used as vaccine adjuvant to enhance innate and adaptive immune responses. |
| M10703 | PF-4878691 | PF-4878691 (3M-852A) is a highly potent, orally active, selective Toll-like receptor 7 (TLR7) agonist that separates its antiviral activity from its inflammatory activity. |
| M10331 | CRX-527 | CRX-527 is a highly specific and potent TLR4 agonist, which displays significantly less toxicity when compared to LPS. |
| M10223 | Okanin | Okanin attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways, it is the effective constituent of the flower tea Coreopsis tinctoria. |
| M9904 | ODN 1826 | ODN 1826 is a class B CpG ODN and an agonist of TLR9, which promotes apoptosis and has antitumor activity. In addition, ODN 1826 induces NO and iNOS production in a mouse model. |
| M9746 | CU-CPT-8m | CU-CPT8m is an antagonist of toll-like receptor 8 (TLR8) with Kd of 220 nM and IC50 of 67 nM in assay. |
| M9742 | CU-CPT-9a | CU-CPT-9a is a potent TLR8 antagonist with IC50 of 0.5 nM, which that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells. |
| M9741 | CU-CPT9b | CU-CPT9b is a potent and selective TLR8 inhibitor, with an IC50 of 0.7 nM. |
| M9692 | IAXO-102 | Iaxo-102 is an antagonist of TLR4 and inhibits the TLR4 signaling pathway. Iaxo-102 inhibits phosphorylation of MAPK and P65 NF-KB and expression of TLR4 and TLR4-dependent inflammatory proteins. Iaxo-102 inhibits the development of experimental abdominal aortic aneurysms. |
| M9651 | TLR4-IN-C34 | C34 is a TLR4 inhibitor, which inhibited TLR4 in enterocytes and macrophages in vitro, and reduced systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis. |
| M9427 | CU-CPT17e | CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist, which activates TLR3, TLR8 and TLR9. |
| M9289 | E6446 dihydrochloride | E6446 dihydrochloride is a synthetic antagonist of TLR7 and TLR9. |
| M9204 | Pam3CSK4 | Pam3CSK4 is a Toll-like receptor 1/2 (TLR1/2) agonist. |
| M8657 | Sparstolonin B | Sparstolonin B (SsnB), an isocoumarin isolated from Sparganium stoloniferum and Scirpus yagara, is a potent TLR2 and TLR4 antagonist that exhibits anti-inflammatory and anti-viral (anti-HIV) properties. |
| M8408 | CU-CPT22 | CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM. |
| M8260 | Bropirimine | Bropirimine is a synthetic agonist of Toll-like receptor 7 (TLR7). Bropirimine inhibits osteoclast differentiation from osteoclast precursor cells through TLR7-mediated IFN-β production. Bropirimine is an oral active immunomodulator with anticancer activity in transitional cell carcinoma in situ (CIS) of the bladder and upper urinary tract. |
| M7408 | TH 1020 | TH1020 is an effective selective toll-like receptor 5 (TLR5)/ flagellin complex antagonist with IC50 of 0.85 μM. TH1020 inhibits flagellin-induced TLR5 signal transduction, but has no effect on TLR2, TLR3, TLR4, TLR7 and TLR8. |
| M7308 | SM 324405 | SM 324405 is a potent TLR7 agonist. |
| M7189 | Resiquimod | Resiquimod is a agonist of Toll-like receptors 7 and 8 (TLR7/TLR8) that induces upregulation of cytokines such as TNF-α, IL-6 and IFN-α. |
| M6246 | TLR7-agonist-1 | TLR7-agonist-1 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM. |
| M5800 | Motolimod (VTX-2337) | Motolimod (VTX-2337) is a selective and potent Toll-like receptor (TLR) 8 agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2. |
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