lipid-lowering

Lipid-lowering agent-1 is a potent lipid-lowering compound that significantly inhibits the pharmacological effects of low-density lipoprotein cholesterol (LDLC) and promotes high-density lipoprotein cholesterol (HDLC) production. In rats on a high-fat diet, it substantially reduces fat.

Ragaglitazar(NNC-61-0029) is a potent dual PPARα and PPARγ agonist that has shown potent lipid-lowering and insulin sensitizing effects in animal models.Ragaglitazar can be used to study type 2 diabetes.

Lovastatin (MK-803) is an HMG-CoA reductase inhibitor (IC50=3.4 nM). Lovastatin lowers cholesterol and is commonly used as a lipid-lowering agent in the treatment of hypercholesterolemia.

Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.

Naringin (Naringoside), a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.

Mevastatin (ML236B) is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum. Mevastatin was the first statin to enter clinical trials.

Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) is a macrocyclic compound utilized as a solubilizer for hydrophobic substances in biological studies, and serves as a lipid raft inhibitor with cholesterol-lowering and potential antitumor activities.

Dihydrocaffeic acid is a metabolite of chlorogenic acid, a well-known antioxidant component with antioxidant, anti-Alzheimer's disease, neuroprotective, arousal and lipid-lowering effects.

Beclobrate (Sgd 24774) is a novel orally available fibric acid derivative that has shown significant lipid and cholesterol-lowering activity in rodents and may be used in the study of primary hyperlipoproteinemia.

Sultosilic acid piperazine salt (A-585) is a novel lipid-lowering compound that can be used to study type IIb familial combined hyperlipidemia.

AZ-1355 is a novel dibenzoxepine derivative with lipid-lowering properties.

1. Eriocitrin (Eriodictyol-7-O-Rutinoside) is powerful antioxidative flavonoid; (1) Prevents oxidative damages caused by acute exercise-induced oxidative stress.(2) Lipid-lowering effects in a rat model of high-fat diet. 2. Dietary Eriocitrin ameliorates diet-induced hepatic steatosis with activation of mitochondrial biogenesis. 3. Eriocitrin and Apigenin were identified as new potent inhibitors of human carbonic anhydrase VA isozyme.

Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM) that inhibits the proliferation and invasiveness of MDA-MB-231 cells, primarily through RhoA inhibition.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

GW 7647 is an effective and highly selective PPARα agonist, the EC 50 values of human PPARα, PPARγ and PPARδ receptors are 6,1100 and 6200 nM, respectively. GW 7647 can reduce the production of nitric oxide in macrophages and has lipid-lowering and anti-inflammatory properties in the body.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

Pedunculoside is extracted from Ilex rotunda Thunb.

Clinofibrate (Lipoclin)(IC50 of 0.47 mM), a lipid-lowering agent, inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR). It is utilized to control high cholesterol and triacylglyceride levels in the blood.

Cetaben, a PPARα-independent peroxisome proliferator, is a non-fibrotic lipid-lowering drug that effectively reduces cholesterol and triglyceride concentrations.

CUDA is an effective soluble cyclohydrolase inhibitor with IC50 of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases the activity of peroxisome proliferator-activated receptor (PPAR) alpha. CUDA may be valuable for the study of cardiovascular diseases.

Bempedoic acid-d4 is a deuterated compound of Bempedoic acid. Bempedoic acid has a CAS number of 738606-46-7. ETC-1002, also known as ESP-55016 and Bempedoic acid, is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid is a regulator of lipid and carbohydrate metabolism.

Etiroxate (CG-635) is a lipid-lowering agent used in hyperlipoproteinemia research [1].

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils, which exhibit lipid-lowering properties. In transgenic mice expressing human ApoA1, a diet containing maritime pine seed oil (MPSO) reduced high-density lipoprotein and ApoA1 levels and diminished cholesterol efflux in vitro. Korean pine seed oil supplements may aid in reducing obesity by decreasing appetite, as evidenced by increased levels of satiety hormones CCK and GLP-1 and reduced desire to eat. Pinolenic acid, which is not metabolically converted to arachidonic acid, can lower arachidonic acid levels in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. The neutral, more lipophilic form of pinolenic acid is pinolenic acid ethyl ester.

CI 924 is a lipid-lowering drug. CI 924 increased anti-atherosclerotic HDL and decreased VLDL at 600 mg/day.

Recaticimab (SHR-1209) is a humanized monoclonal antibody targeting PCSK9 to enhance its degradation. By binding to PCSK9, Recaticimab elevates low-density lipoprotein (LDL) receptor presence on hepatocyte surfaces, consequently lowering plasma LDL levels and aiding in blood lipid reduction. This positions Recaticimab as a promising therapeutic for hypercholesterolemia [1] [2].

Gemcabene calcium , a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) andexerting anti-inflammatory activity, lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP).

6-Raloxifene-β-D-glucopyranoside is a benzothiophene glucuronidated at the 6' position. It is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss, resorption, and lowering lipid

12-methyl Myristic acid methyl ester is a methylated fatty acid methyl ester that has been found in vermicomposts of cattle manure, carica papaya leaves, and cuticular wax of K. africana. It is a volatile compound in lipid-lowering granulated tea. Levels of 12-methyl myristic acid methyl ester are decreased in T. cruzi treated with nifurtimox compared to non-treated controls.

Gemcabene (PD-72953) is a lipid-lowering agent with anti-inflammatory activity. Gemcabene lowers low-density lipoprotein cholesterol and triglycerides, raises high-density lipoprotein cholesterol, and decreases pro-inflammatory acute-phase protein, C-reactive protei

Muraglitazar glucuronide is a Peroxime Proliferator Activated (PPAR) Agonist that has glucose- and lipid-lowering activities.

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro.[1] Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an increase in the satiety hormones CCK and GLP-1 and a reduced desire to eat.[2] The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not converted to arachidonic acid metabolically and can reduce arachidonic acid levels in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%.[3]

Total panax notoginsenosides (TPNS) are the main active ingredients in San-Chi, the root of(Burk) F.H. Chen, which belongs to the Araliaceae family and has been used in traditional Chinese medicine to treat atherosclerosis;TPNS can prevent atherosclerosis

PPAR agonist 1 is a dual PPAR α γ agonist used for lowering blood glucose, lipid levels, cholesterol, and body weight.

BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of animal, plant, and fungal sterols.

Flavanomarein demonstrates potent antioxidative property, including free radical scavenging activity, inhibition of lipid peroxidation, as well as lipid-lowering effects in human HepG2 hepatocellular carcinoma cells treated with free fatty acids (FFAs).

BAY-02752 is a lipid lowering agent that has been shown in rats to inhibit the absorption of intestinal cholesterol.

K 13-004 is a lipid-lowering agent.

RP 54275 is a naturally occurring fatty acid derivative, a new cholesterol-lowering compound. It activates the peroxisome proliferator-activated receptor gamma (PPARγ) pathway, which is involved in the regulation of lipid metabolism, inflammation and cellular differentiation.

Lerodalcibep (LIB003), a lipid-lowering agent, consists of a PCSK9-binding domain (adnectin) fused with human serum albumin, forming a recombinant fusion protein. It is utilized in the research of hypercholesterolemia and cardiovascular diseases [1].

Ongericimab (JS002) is a humanized monoclonal antibody targeting PCSK9, demonstrating lipid-lowering efficacy, and is used in research on hypercholesterolemia and hyperlipidemia [1].

Bempedoic acid (ETC1002) is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid(ETC1002) is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid(ETC1002) is a regulator of lipid and carbohydrate metabolism.

Etiroxate, (S)- has a lipid-lowering effect.

Febuprol, a choleretic drug, stimulates bile secretion. In addition, it also has lipid-lowering (lowering blood lipid) and spasmolytic (anticonvulsant) properties.

17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.

Lapaquistat is a cholesterol biosynthesis inhibitor and is the active metabolite of TAK-475. Lapaquistat can reduce statin-induced myotoxicity in lipid-lowering therapy.

Bemfivastatin hemicalcium (PPD 10558), an orally active HMG-CoA reductase inhibitor, serves as a lipid-lowering agent. It amplifies liver extract activity and exhibits no-observed adverse effect levels (NOAEL) at dosages of ≥320 mg/kg/d for rat developmental toxicity, ≥12.5 mg/kg/d for rabbit maternal toxicity, and ≥25 mg/kg/d for rabbit developmental toxicity. This compound is utilized in research concerning hypercholesterolemic myalgia in patients intolerant to statins.

GW 9578 is a selective and potent PPARα agonist with potent lipid-lowering activity for the study of psoriasis, arthritis, alopecia, asthma and type I diabetes.

Linerixibat (GSK2330672) is a highly effective, nonabsorbable ASBT inhibitor (IC50: 42 ± 3 nM) that can lower glucose in an animal model of type 2 diabetes and demonstrates excellent developability properties.

F44-A13 is an orally active, highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. It optimizes cholesterol metabolism and reduces activity by inducing CYP7A1 expression, lowering cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) levels in mouse models. F44-A13 is applicable for studying metabolic diseases associated with lipid disorders [1].