PCSK9

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  1. PCSK9 antagonist

    SBC-115076 is an anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds, for the treatment and/or prevention of cardiovascular diseases.
  2. PCSK9 inhibitor

    SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1, Figure 1.
  3. anti-secretagogue of PCSK9

    R-IMPP is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
  4. PCSK9 inhibitor

    PF-06446846 hydrochloride is an orally active and highly selective inhibitor of the translation of proprotein convertase subtilisin/kexin type 9 (PCSK9). It inhibits PCSK9 expression by inducing ribosomal stalling at approximately codon 34 during translation.
  5. PCSK9 inhibitor

    AZD0780 (PCSK9-IN-12) is a heteroaryl compound with high binding affinity for proprotein convertase subtilisin/kexin type 9 (PCSK9), exhibiting a Kd value of <200 nM. It is a valuable tool for research in cholesterol metabolism and PCSK9-related therapeutic pathways.
  6. PCSK9 Inhibitor

    Inclisiran is a double-stranded small interfering RNA (siRNA) that specifically targets and inhibits the transcription of proprotein convertase subtilisin/kexin type 9 (PCSK9). By reducing PCSK9 levels, Inclisiran effectively modulates lipid metabolism and demonstrates anti-inflammatory properties, including the inhibition of pyroptosis and a decrease in NLRP3, cleaved caspase-1, IL-1β, and IL-18. This reagent is valuable for research applications focused on hyperlipidemia and cardiovascular diseases (CVD), as it supports studies aimed at understanding lipid regulation and atherosclerosis.
  7. PCSK9 Inhibitor

    Pinostrobin is a flavonoid that acts as a potent inhibitor of PCSK9, targeting its catalytic activity. This compound demonstrates significant anti-cancer, antioxidant, antiviral, and neuroprotective properties. Pinostrobin is suitable for research applications in diverse areas, including viral infections, cancer therapeutics, cardiovascular and cerebrovascular disorders, cirrhosis, inflammatory diseases, and neurological conditions.
  8. PCSK9 ATTEC

    PCSK9 autophagic degrader 2 (W6) targets proprotein convertase subtilisin/kexin type 9 (PCSK9) through an autophagic mechanism, displaying a DC50 value of 20.6 nM. This compound exhibits significant antiatherosclerotic activity, with a dissociation constant (KD) for LC3B of 2.5 μM. PCSK9 autophagic degrader 2 (W6) facilitates research into cholesterol homeostasis, cardiovascular disease, and potential therapeutic interventions targeting the PCSK9 pathway.
  9. PCSK9 Inhibitor

    DC371739 is a potent PCSK9 inhibitor that exhibits oral bioactivity. It effectively reduces the mRNA expression of both PCSK9 and ANGPTL3, while simultaneously increasing the protein expression of LDLR. This compound holds promise for research applications related to hyperlipidemia and the modulation of lipid metabolism.
  10. PCSK9 Inhibitor

    MeIm is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) that acts as a peptide mimetic. It effectively enhances the cellular uptake of low-density lipoprotein (LDL) with an EC50 value of 6.04 μM by disrupting the interaction between PCSK9 and LDL receptors (LDLR), with an IC50 of 11.2 μM. MeIm is valuable for research focused on cardiovascular diseases and related lipid metabolism studies.
  11. PCSK9 Inhibitor

    BRD8518 is a potent inhibitor of PCSK9, exhibiting an EC50 of 0.23 μM. By upregulating LDLR expression, BRD8518 effectively lowers blood lipid levels and enhances LDL uptake. This compound is valuable for research applications focused on cardiovascular diseases, facilitating the exploration of lipid metabolism and associated therapeutic strategies.
  12. PCSK9/HMG-CoAR Inhibitor

    Dim16 is a dual inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) and HMG-CoA reductase (HMG-CoAR), demonstrating an IC50 value of 19 nM for PCSK9. It effectively inhibits the binding of PCSK9 to the LDL receptor (LDLR) with an IC50 of 0.8 nM. This compound is noted for its role in enhancing LDL uptake in HepG2 cells, making it valuable for research in cholesterol metabolism and cardiovascular diseases.
  13. PCSK9 antagonist

    Enlicitide chloride is a potent orally active antagonist of PCSK9, inhibiting the interaction between the lipoprotein lipase (LPL) receptor and PCSK9 with an IC50 of 2.5 nM. This compound is invaluable for investigating cardiovascular diseases, including atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, and acute coronary syndrome, as well as other related cardiometabolic disorders. Researchers may utilize Enlicitide chloride to explore therapeutic strategies targeting lipid metabolism and cardiovascular health.
  14. PCSK9 Inhibitor

    PCSK9-IN-34 is a small molecule inhibitor targeting proprotein convertase subtilisin/kexin type 9 (PCSK9). It plays a crucial role in regulating cholesterol levels by preventing PCSK9-mediated degradation of LDL receptors. This compound is valuable for research into cardiovascular conditions and cholesterol metabolism, particularly in the context of hyperlipidemia and atherosclerosis.
  15. PCSK9/IDLR/SREBP2 mRNA Inhibitor

    5-O-Methylembelin is a natural isocoumarin that functions as an inhibitor of PCSK9, the inducible degrader of the low-density lipoprotein receptor (IDLR), and SREBP2 mRNA expression. This compound is essential for studying lipid metabolism and cholesterol regulation, making it valuable for research focused on hypercholesterolemia and cardiovascular diseases. Its ability to modulate these crucial pathways enables exploration of potential therapeutic strategies targeting lipid homeostasis.
  16. PCSK9 Inhibitor

    PCSK9-IN-10 is a potent oral inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibiting an IC50 value of 6.4 µM. This compound enhances the expression of LDL receptors (LDLR) while downregulating PCSK9 levels, contributing to the reduction of atherosclerosis progression. PCSK9-IN-10 is suitable for research applications focused on hyperlipidemia and cardiovascular diseases.
  17. PCSK9 Inhibitor

    PCSK9-IN-11 is a potent, orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It demonstrates effective transcriptional inhibitory activity in HepG2 cells, with an IC50 value of 5.7 μM. By increasing the protein level of LDL receptors (LDLR), PCSK9-IN-11 serves as a valuable tool for research in atherosclerosis and lipid metabolism.
  18. PCSK9 inhibitor

    PCSK9-IN-23 is a potent inhibitor of PCSK9, effectively blocking its secretion from HepG2 cells. This inhibition leads to a significant increase in LDL receptor (LDLR) expression, making it valuable for research aimed at understanding lipid metabolism and developing therapeutic strategies for hyperlipidemia and cardiovascular diseases. Its ability to modulate LDLR provides insights into cholesterol regulation and potential interventions in related disorders.
  19. PCSK9 Inhibitor

    PCSK9-IN-13 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), significantly disrupting its interaction with low-density lipoprotein (LDL) receptors. With an IC50 value of 537 nM, this compound is instrumental in studying lipid metabolism and cardiovascular diseases. Its application in research can facilitate the development of novel therapeutics for disorders associated with dyslipidemia.
  20. PCSK9 Inhibitor

    SBC-115337 is a potent PCSK9 inhibitor, demonstrating an IC50 value of 0.5 μM. By targeting proprotein convertase subtilisin/kexin type 9 (PCSK9), this compound plays a critical role in modulating cholesterol metabolism. SBC-115337 is suitable for research applications aimed at studying lipid metabolism, cardiovascular diseases, and the development of therapies for hypercholesterolemia.
  21. PCSK9 Inhibitor

    PF-06815345 hydrochloride is a potent, orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), demonstrating an IC50 of 13.4 μM. This compound effectively reduces PCSK9 levels in vivo in mouse models, making it a valuable tool for research into lipid metabolism and cardiovascular disease. Its role as a PCSK9 inhibitor positions it for studies aimed at exploring cholesterol regulation and related therapeutic interventions.
  22. PCSK9 Inhibitor

    PF-06446846 is an orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). This compound selectively targets PCSK9 translation by stalling the 80S ribosome near the codon region, effectively reducing PCSK9 levels. It has significant implications in research related to cholesterol metabolism and cardiovascular diseases, making it a valuable tool for investigations into lipid regulation and associated therapeutic strategies.
  23. PCSK9 Antagonist

    E28362 is a selective PCSK9 antagonist that functions as an orally active lipid-lowering agent. By inhibiting the interaction between PCSK9 and the LDL receptor (LDLR), E28362 promotes the degradation of PCSK9 through the ubiquitin-proteasome pathway, leading to increased cell surface and total levels of LDLR. This mechanism enhances low-density lipoprotein uptake, resulting in significant reductions in plasma lipids, hepatic cholesterol, and triglyceride levels. E28362 also demonstrates minimal cytotoxicity at high concentrations and has been shown to substantially reduce atherosclerotic lesions in animal models, making it a valuable tool in studies of hyperlipidemia and atherosclerosis.
  24. PCSK9 Inhibitor

    PF-06815345 is a potent and orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), exhibiting an IC50 value of 13.4 μM. This compound has been shown to significantly reduce PCSK9 levels in vivo in mouse models. PF-06815345 serves as a valuable tool for studying cholesterol metabolism and the modulation of LDL receptor activity, making it relevant for research in cardiovascular diseases and lipid regulation.
  25. PCSK9 Inhibitor

    7030B-C5 is a potent PCSK9 inhibitor with an IC50 of 1.61 μM. This compound effectively reduces plasma cholesterol and triglyceride levels in vivo, contributing to the attenuation of atherosclerosis progression. 7030B-C5 serves as a valuable tool in cardiovascular disease research, facilitating the exploration of lipid metabolism and associated therapeutic strategies.
  26. PCSK9 Inhibitor

    Bezeparsen is a potent PCSK9 synthesis inhibitor that regulates LDL cholesterol levels by enhancing hepatic LDL receptor activity. It plays a critical role in lipid metabolism and is used in cardiovascular research to study cholesterol homeostasis and potential therapeutic interventions for hyperlipidemia. This compound is valuable for investigations focusing on the modulation of cholesterol levels and cardiovascular disease management.
  27. PCSK9 Inhibitor

    PCSK9 modulator-2 is a potent inhibitor of PCSK9, exhibiting an EC50 value of 202 nM. PCSK9 plays a critical role in the regulation of low-density lipoprotein cholesterol (LDL-C) levels in the blood. This modulator presents valuable utility in research focused on hyperlipidemia and cholesterol metabolism, offering insights into potential therapeutic strategies for managing lipid disorders.
  28. PCSK9 Inhibitor

    PCSK9-IN-16 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). By inhibiting PCSK9, this compound plays a crucial role in regulating cholesterol levels, making it relevant for research into hypercholesterolemia and other cardiovascular diseases. It offers a valuable tool for studies focused on lipid metabolism and potential therapeutic interventions in lipid disorders.
  29. PCSK9 Inhibitor

    SPC4061 is a potent PCSK9 inhibitor that utilizes an antisense nucleotide mechanism. By specifically targeting the locked nucleic acid (LNA) of PCSK9, it plays a crucial role in the study of hypercholesterolemia and associated metabolic disorders. This compound enables researchers to explore the regulation of cholesterol metabolism and related therapeutic approaches.
  30. PCSK9 Ligand

    PCSK9 ligand 1 is a selective ligand for proprotein convertase subtilisin/kexin type 9 (PCSK9), which plays a critical role in cholesterol metabolism and regulation. This compound does not interfere with the functional activity of PCSK9, making it a valuable tool for studying PCSK9 interactions and cholesterol homeostasis. It is applicable in research focused on lipid metabolism, cardiovascular diseases, and potential therapeutic interventions targeting PCSK9 pathways.
  31. PCSK9 Inhibitor

    PCSK9 modulator-3 is a potent inhibitor of PCSK9, exhibiting an EC50 value of 2.46 nM. By targeting PCSK9, this compound facilitates the reduction of low-density lipoprotein cholesterol (LDL-C) levels. PCSK9 modulator-3 is valuable for research into hyperlipidemia and potential therapeutic strategies for managing cholesterol-related disorders.
  32. PCSK9 Degrader

    (R,R)-PCSK9 degrader 1 targets proprotein convertase subtilisin/kexin type 9 (PCSK9) and functions as a potent small molecule degrader. With a high affinity (Ki = 107 nM), it effectively disrupts the interaction between PCSK9 and low-density lipoprotein (LDL) receptors. This compound is valuable for research applications focused on cholesterol metabolism and cardiovascular diseases, enabling investigations into the modulation of lipid profiles and potential therapeutic interventions.
  33. PCSK9 Inhibitor

    PCSK9-IN-18 is a potent inhibitor of PCSK9, demonstrating a KD value of less than 200 nM. By targeting PCSK9, this compound plays a critical role in modulating LDL receptor levels and lipid metabolism. It is valuable for research in cardiovascular diseases and the development of therapies aimed at lowering cholesterol levels.
  34. PCSK9 Inhibitor

    PCSK9-IN-22 is a potent orally active inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). This compound effectively disrupts the interaction between PCSK9 and low-density lipoprotein receptor (LDLR), leading to increased LDLR levels and enhanced clearance of LDL cholesterol. PCSK9-IN-22 is valuable for research applications related to cholesterol metabolism, cardiovascular disease, and lipid regulation.
  35. PCSK9 Inhibitor

    PCSK9-IN-26 is a potent inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) with an IC50 value of less than 1 nM. This compound effectively modulates lipid metabolism by preventing PCSK9-mediated degradation of LDL receptors, thereby promoting cholesterol uptake. PCSK9-IN-26 is valuable for research applications focused on cardiovascular diseases and metabolic disorders related to cholesterol homeostasis.
  36. PCSK9 Inhibitor

    PCSK9-IN-31 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). This compound effectively lowers low-density lipoprotein cholesterol (LDL-C) and total cholesterol (TC) levels in high cholesterol-fed rat models. It is valuable for research applications focused on cholesterol metabolism and cardiovascular disease.
  37. PCSK9 Inhibitor

    PCSK9-IN-14 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). By targeting PCSK9, this compound effectively enhances LDL receptor degradation and promotes lipid metabolism. It serves as a valuable tool for research into cholesterol metabolism and the development of therapies for hypercholesterolemia.
  38. PCSK9 Inhibitor

    PCSK9-IN-17 is a selective inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), targeting the regulation of cholesterol metabolism. This compound has demonstrated efficacy in modulating LDL receptor levels, thereby enhancing lipid homeostasis. PCSK9-IN-17 is primarily utilized in research focused on cholesterol metabolism and cardiovascular disease mechanisms, providing valuable insights into therapeutic strategies for dyslipidemia and related disorders.
  39. Anti-PCSK9 Antibody

    Ticalicibart is a humanized IgG4κ monoclonal antibody that selectively inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). By targeting PCSK9, Ticalicibart demonstrates significant anti-hyperlipidaemic activity, making it a valuable tool for research in cardiovascular diseases, particularly hypercholesterolaemia. Its applications extend to elucidating the mechanisms underlying lipid metabolism and exploring novel therapeutic approaches for managing cholesterol levels.
  40. PCSK9 Inhibitor

    PCSK9-IN-24 is a potent inhibitor of PCSK9, a key regulator of LDL receptor degradation. By reducing PCSK9 levels, this compound facilitates increased LDL uptake by cells, making it valuable for investigations into cholesterol metabolism and atherosclerosis. Its application in research can enhance the understanding of lipid disorders and aid in the development of therapeutic strategies targeting cardiovascular diseases.
  41. PCSK9 Inhibitor

    PCSK9 modulator-4 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), exhibiting an EC50 value of 0.15 nM. By targeting PCSK9, this compound plays a crucial role in reducing low-density lipoprotein cholesterol (LDL-C) levels. PCSK9 modulator-4 is particularly relevant for research focused on hyperlipidemia and related cardiovascular diseases.
  42. PCSK9 Inhibitor

    PCSK9-IN-15 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), with a known dissociation constant (KD) of less than 200 nM. PCSK9 plays a critical role in cholesterol metabolism, primarily regulating low-density lipoprotein cholesterol (LDL-C) levels in the bloodstream. This compound is valuable for investigating cholesterol-lowering effects and the mechanisms underlying dyslipidemia.
  43. PCSK9

    Cepadacursen sodium is an antisense oligonucleotide (ASO) that targets and inhibits the synthesis of proprotein convertase subtilisin/kexin type 9 (PCSK9) in the liver. By reducing PCSK9 levels, it plays a critical role in regulating cholesterol metabolism. This reagent is particularly relevant for research focused on hypercholesterolemia and the prevention strategies for atherosclerotic cardiovascular disease (ASCVD).
  44. PCSK9 allosteric binder

    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.
  45. PCSK9 Inhibitor

    PCSK9-IN-20 is a potent PCSK9 inhibitor with an IC50 of 3.96 µM. This compound effectively reduces PCSK9 levels and upregulates LDL receptor (LDLR) expression in vitro. It serves as a valuable tool for research applications focused on cholesterol metabolism and cardiovascular disease mechanisms.
  46. PCSK9 siRNA

    AZD8233 is an antisense oligonucleotide (ASO) that targets proprotein convertase subtilisin/kexin type 9 (PCSK9) to inhibit its protein synthesis. By reducing levels of PCSK9, AZD8233 enhances the availability of LDL receptors, which facilitates the clearance of low-density lipoprotein (LDL) from circulation and contributes to lowering LDL cholesterol (LDL-C) levels. This compound is applicable in research focused on lipid metabolism and cardiovascular disease.

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