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PCSK9

PCSK9 inhibitors and degraders target a secreted protein that limits cholesterol uptake by the liver. Proprotein convertase subtilisin/kexin type 9 (PCSK9) was described in 2003 as neural apoptosis-regulated convertase 1 (NARC-1), a convertase expressed in liver and brain. In the same year, mutations in its gene were linked to autosomal dominant hypercholesterolemia. Secreted PCSK9 binds low-density lipoprotein (LDL) receptors and routes them to lysosomal degradation. SBC-115076 and laroprovstat are small-molecule PCSK9 inhibitors, while PF-06446846 hydrochloride selectively stalls ribosomes during PCSK9 translation. Inclisiran is a small interfering RNA (siRNA), and PCSK9 autophagic degrader 2 removes the protein through autophagy.

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  • PCSK9 allosteric binder-1
    Cat. No.
    A77061
    CAS No.
    2215932-06-0

    PCSK9 allosteric binder-1

    PCSK9 allosteric binder-1 is a novel allosteric modulator of proprotein convertase subtilisin/kexin type 9 (PCSK9). This compound effectively modifies the interaction between PCSK9 and its receptor, leading to increased LDL receptor degradation. It holds significant potential for research applications in understanding and treating cardiovascular diseases, particularly those related to lipid metabolism and cholesterol homeostasis.

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