HYDROPHILIC SILICON-RHODAMINE FLUORESCENT PROBES AND USE THEREOF

    公开(公告)号:US20200340920A1

    公开(公告)日:2020-10-29

    申请号:US16860540

    申请日:2020-04-28

    Abstract: The present invention relates to a novel near-infrared fluorescent probe having specificity for mitochondria due to a hydrophobic group attached to a silicon-rhodamine core, and the use thereof for mitochondrial detection and cancer diagnosis. The fluorescent probe of the present invention has improved mitochondrial targeting efficiency compared to conventional probes due to a hydrophobic group attached to a silicon-rhodamine core, can detect mitochondria in living tissue with high sensitivity and specificity in a near-infrared (NIR) region (700 to 1,700 nm), and can acquire three-dimensional high-resolution biological images without harming the human body. Due to these advantages, the fluorescent probe can be used not only for mitochondrial detection in cells in the laboratory, but also as a contrast agent or a drug delivery carrier in cancer diagnosis and surgery.

    SMALL MOLECULE ANTAGONIST COMPOUND TAC5 SERIES HAVING TOLL-LIKE RECEPTOR 3/7/8/9 INHIBITORY FUNCTION

    公开(公告)号:US20210214372A1

    公开(公告)日:2021-07-15

    申请号:US17057967

    申请日:2019-05-20

    Abstract: A small molecule antagonist compound having a toll-like receptor 3/7/8/9 inhibitory function and its use in inhibiting TLR7, TLR8, TLR9 and TLR3 are disclosed. A novel compound expressed by TAC5 and TAC5-a, TAC5-c, TAC5-d or TAC5-e which are derivatives thereof not only prevents TNFα secretion, NFkB activation, IkB degradation and MAPKs phosphorylation induced by poly(I:C) (TLR3 agonist), IMQ (TLR7 agonist), CL075 (TLR7/8 agonist), R848 (TLR7/8 agonist), TL8 (TLR8 agonist) or CpG ODN (TLR9 agonist), but also inhibits generation of inflammatory cytokine, and thus is highly advantageous for preventive or therapeutic use for TLR3/7/8/9-related autoimmune diseases and inflammatory diseases including systemic lupus erythematosus, psoriasis and the like.

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