CU-115 是一种强有力的 TLR8 拮抗剂 (IC₅₀=1.04 µM)，并显示了对 TLR8 选择性高于TLR7 (IC₅₀=>50 µM)。CU-115 降低了由 R-848 激活的 THP-1 细胞 TNF-α 和 IL-1β 的产生。

CU-115 is a potent TLR8 antagonist (IC 50 =1.04 μM), and shows selective for TLR8 over TLR7 (IC 50 =>50 μM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.

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TLR8 1.04 μM (IC50) TLR7 50 μM (IC50

In endosomal and non-endosomal TLR specificity studies, Human embryonic kidney (HEK) 293 cells expressing human tolllike receptor (hTLR) gene and an inducible secreted embryonic alkaline phosphatase (SEAP) reporter gene were incubated with CU-115 for 16 hours. As a result, CU-115 displays activity for TLR7 and TLR8 at low concentrations (0.5 μM).
CU-115 does not modulate the NF-kB inhibition induced by Pam2CSK4, Pam3CSK4, Poly(I:C), LPS, R848, and Flic in HEK-293 TLR1/2, TLR2/6, TLR3, and TLR4 cells. And CU-115 inhibits TLR9 signaling at 1, 5, and 20 μM and ~10-25% inhibition.
CU-115 (5-20 μM) inhibits increases in type I IFN transcriptional activity induced by the ssRNA nucleic acid ligands 3p-hpRNA or G3-YSD in a luciferase reporter assay.
CU-115 (0.5, 1.0, 5, and 20 μM; 16 hours) is nontoxic at low concentrations (0.5 and 20 μM) and toxic at 100 μM in Hek293 TLR7 a

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[1]. Rosaura Padilla-Salinas, et al. Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors 7 and 8. J Med Chem. 2019 Nov 27;62(22):10221-10244.

In Vitro: DMSO : 100 mg/mL (175.68 mM; Need ultrasonic)配制储备液