Hypercholesterolemia

Gypenoside LVI is an orally active dammarane-type triterpenoid compound found in Gynostemma pentaphyllum. Gypenoside LVI inhibits ERK and JNK phosphorylation, the NLRP3 inflammasome, and modulates M1 to M2 microglial polarization. Gypenoside LVI downregulates PCSK9 expression through a SREBP-independent pathway. Gypenoside LVI promotes cholesterol efflux via ABCG1 and SRB1, upregulates LXRα-mediated reverse cholesterol transport, and attenuates foam cell formation by reducing lipid accumulation and cholesterol uptake. Gypenoside LVI inhibits IL-6 and IL-1β secretion, reduces oxidative stress, neuroinflammation, microglial and astrocyte activation, and inhibits LPS-induced microglial proliferation. Gypenoside LVI can be used for research on atherosclerosis, hypercholesterolemia, depression, and non-small cell lung cancer.

Azalanstat (RS-21607) mesylate is an orally active lanosterol 14α-demethylase inhibitor. Azalanstat mesylate exerts a cholesterol-lowering effect by inhibiting cholesterol synthesis and regulating HMG-CoA Reductase (HMGCR), and shows an additive effect when used in combination with Cholestyramine (HY-104081). Azalanstat mesylate is used in the study of hypercholesterolemia.

R-IMPP hydrochloride (PF-00932239 hydrochloride) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP hydrochloride inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP hydrochloride reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP hydrochloride increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP hydrochloride inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP hydrochloride can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia.

Mdl 28815 is an inhibitor of Sterol-delta 14-reductase and 2,3-oxido-squalene cyclase, with IC₅₀ values of 0.07 μM and 2 μM, respectively. Mdl 28815 blocks cholesterol biosynthesis and causes the accumulation of specific sterol metabolites. Mdl 28815 is applicable to research related to hypercholesterolemia.

Boxidine is an orally active DHCR7 inhibitor. Boxidine inhibits DHCR7, blocks the conversion of 7-Dehydrocholesterol (HY-113279) to Cholesterol (HY-N0322), reduces serum cholesterol levels, causes accumulation of 7-dehydrocholesterol in serum and tissues, and inhibits sterol absorption. Boxidine exhibits antiproliferative and anticancer activities, with marginal activity against mouse tumors. Boxidine can be used in research related to diseases such as tumors and adrenal cancer.

Dim16 hydrochloride is a dual PCSK9 inhibitor and HMG-CoAR inhibitor, with an IC₅₀ of 0.8 nM against human PCSK9 and an IC₅₀ of 146.8 μM against HMG-CoAR. Dim16 hydrochloride disrupts the PCSK9-LDLR protein-protein interaction, inhibits the catalytic activity of HMG-CoAR, enhances cellular uptake of extracellular LDL, and suppresses PCSK9-induced platelet aggregation. Dim16 hydrochloride can be used in research related to hypercholesterolemia.

ABCA1 inducer 3 (Compound 85) is an orally active ABCA1 inducer and lipid-modulating agent. ABCA1 inducer 3 increases ABCA1 expression. ABCA1 inducer 3 upregulates hepatic Abcg5 and Abcg8 mRNA expression. ABCA1 inducer 3 promotes cholesterol efflux. ABCA1 inducer 3 improves hyperlipidemia.

Terbufibrol (Standard) is the analytical standard of Terbufibrol (HY-101812). This product is intended for research and analytical applications. Terbufibrol is an orally active lipid-lowering agent. Terbufibrol inhibits hepatic Cholesterol 7 alpha-hydroxylase. Terbufibrol blocks a step between Acetate and HMG-CoA in the hepatic cholesterol synthesis process. Terbufibrol reduces serum total cholesterol, HDL, LDL, lipoprotein levels, and the cholesterol/phospholipid ratio, with dose- and sex-dependent changes in lipoprotein components. Terbufibrol exerts sustained cholesterol-lowering activity in baboons and rats. Terbufibrol can be used in research related to hypercholesterolemia.