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cardiometabolic disease

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By Targets:	Apelin Receptor (APJ) (1) Arrestin (1) Endogenous Metabolite (4) Epoxide Hydrolase (1) FAAH (1) PCSK9 (1) PDHK (1) Phospholipase (1) Thyroid Hormone Receptor (1)
By Research Areas:	Cardiovascular Disease (7) Metabolic Disease (5)

10

Inhibitors & Agonists

1

Peptides

4

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

Enlicitide chloride MK-0616 chloride	PCSK9	Cardiovascular Disease
Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC₅₀ of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders .

PF-07247685	Endogenous Metabolite	Cardiovascular Disease
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC₅₀=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .

1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine SLPC; 18:0-18:2 PC	Endogenous Metabolite	Cardiovascular Disease Metabolic Disease
1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine (SLPC; 18:0-18:2 PC) is an endogenous phospholipid marker molecule in the glycerophospholipid metabolic pathway. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine is a core component of the phospholipid bilayer of biological membranes and a key responsive lipid for radiation injury and cardiometabolic diseases. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine constitutes the phospholipid bilayers of cell membranes and high-density lipoprotein (HDL), and regulates the core activity of lipoprotein functional homeostasis. The content of 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine in mouse serum shows a significant dose-dependent decrease with increasing ionizing radiation dose, and its level in human HDL also decreases significantly in metabolic syndrome. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can serve as a biological dosimeter marker for ionizing radiation injury, and is used for rapid and accurate assessment of radiation absorbed dose in exposed individuals. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can also act as a lipidomics research target for cardiometabolic diseases such as lipid metabolic syndrome and early-onset coronary heart disease .

PF-07208254	PDHK	Cardiovascular Disease Metabolic Disease
PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC₅₀=110 nM, K_i=54 nM, K_D=84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC₅₀=540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes) .

VU534	FAAH Epoxide Hydrolase	Cardiovascular Disease
VU534 is a NAPE-PLD activator, with an EC₅₀ of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC₅₀ of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study ^[1].

VU533 1 Publications Verification	Phospholipase	Metabolic Disease
APE-PLD (VU533) activator is a potent NAPE-PLD activator with an EC₅₀ value of 0.30 µM. NAPE-PLD activator (VU533) can enhance NAPE-PLD activity and increase efferocytosis by macrophages. NAPE-PLD activator (VU533) can be used for cardiometabolic diseases research .

APJ receptor agonist 6	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with K_i of 1.3 μM. APJ receptor agonist 6 has EC₅₀ values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively .

PF-07238025	Endogenous Metabolite	Cardiovascular Disease
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC₅₀=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .

THRβ receptor agonist-2	Thyroid Hormone Receptor	Metabolic Disease
THRβ receptor agonist-2 (Example 7-4) is a THRβ receptor agonist. THRβ receptor agonist-2 can be used for research of liver disorder or a cardiometabolic disease .

BDK-IN-1	Endogenous Metabolite	Metabolic Disease
BDK-IN-1 (compound (-)-43) is a BDK inhibitor with the IC₅₀ of 0.23 μM and the max inhibition of 90%. BDK-IN-1 decreases the level of phospho-E1 and can be used for study of cardiometabolic diseases .

Cat. No.	Product Name	Target	Research Area

Enlicitide chloride MK-0616 chloride	PCSK9	Cardiovascular Disease
Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC₅₀ of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders .

Cat. No.	Product Name	Category	Target	Chemical Structure

PF-07247685	Cardiovascular Disease Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC₅₀=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .

1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine SLPC; 18:0-18:2 PC	Structural Classification Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Lipid Source Classification	Endogenous Metabolite
1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine (SLPC; 18:0-18:2 PC) is an endogenous phospholipid marker molecule in the glycerophospholipid metabolic pathway. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine is a core component of the phospholipid bilayer of biological membranes and a key responsive lipid for radiation injury and cardiometabolic diseases. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine constitutes the phospholipid bilayers of cell membranes and high-density lipoprotein (HDL), and regulates the core activity of lipoprotein functional homeostasis. The content of 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine in mouse serum shows a significant dose-dependent decrease with increasing ionizing radiation dose, and its level in human HDL also decreases significantly in metabolic syndrome. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can serve as a biological dosimeter marker for ionizing radiation injury, and is used for rapid and accurate assessment of radiation absorbed dose in exposed individuals. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can also act as a lipidomics research target for cardiometabolic diseases such as lipid metabolic syndrome and early-onset coronary heart disease .

PF-07208254	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification	PDHK
PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC₅₀=110 nM, K_i=54 nM, K_D=84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC₅₀=540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes) .

PF-07238025	Cardiovascular Disease Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC₅₀=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .

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