| 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:polycytidylic acid | Polyinosinic: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. |
| 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 (R-848) 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. R848 (Resiquimod) induces differential TLR7 and/or TLR8 responses in human and murine immune cells. R848 (Resiquimod) acts as a selective activating ligand for both TLR7 and TLR8 in humans but only TLR7 in mice. It activates immune cells via the TLR7/TLR8 MyD88-dependent signaling pathway with the subsequent activation of the transcription factors NF-κB and interferon regulatory factor (IRF). |
| 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. |
| M5105 | MD2-TLR4-IN-1 | MD2-TLR4-IN-1 is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. |
| M4539 | Polygalasaponin-F | Polygalasaponin F is an oleanane type triterpenoid saponin extracted from Polygala Japonica, which can reduce the release of inflammatory cytokine tumor necrosis factor α (TNFa). Polygalasaponin F reduces the secretion of neuroinflammatory cytokines by regulating the TLR4-PI3K/ Akt-NF-KB signaling pathway. |
| M4519 | Procyanidin-B1 | Procyanidin B1 is a polyphenolic flavonoid that exists in common fruits and can bind to TLR4/MD-2 complex, showing anti-inflammatory activity. |
| M4341 | Schaftoside | Schaftoside is a flavonoid found in a variety of Chinese herbs such as Eleusine indica. Schaftoside inhibited TLR4 and Myd88 expression. Schaftoside also reduced Drp1 expression and phosphorylation, and reduced mitochondrial division. |
| M4288 | Atractylenolide I | Atractylenolide I is a sesquiterpene obtained from the roots of Atractylenolide. Atractylenolide I has neuroprotective, anti-allergic, anti-inflammatory and anticancer activities. Atractylenolide I is an antagonist of TLR4 and can also reduce the phosphorylation of JAK2 and STAT3 in A375 cells. |
| M2728 | Vesatolimod (GS-9620) | Vesatolimod (GS-9620) is an effective, selective, oral toll-like receptor 7 (TLR7) agonist with an EC50 value of 291 nM. |
| M58213 | CAY10614 | CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. |
| M56410 | BNT411 | BNT411 is a selective TLR7 agonist that can induce the release of IFNa both in vivo and in vitro. |
| M56409 | Rabeximod | Rabeximod (ROB-803), an anti-rheumatic compound, impairs the differentiation and function of human pro-inflammatory dendritic cells and macrophages via downregulating TLR2 and TLR4 stimulation. |
| M56408 | NCI126224 | NCI126224 is a TLR4 signaling inhibitor. |
| M56407 | Afimetoran | Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. |
| M56406 | TLR7/8-IN-1 | TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor. |
| M56405 | Ruzotolimod | Ruzotolimod is the agonist of TLR7. |
| M54728 | Kdo2-Lipid A ammonium | Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxic activity equivalent to LPS.Kdo2-Lipid A ammonium is highly selective for TLR4 and stimulates the release of TNF and PGE2. |
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