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Cardiovascular System

Cardiovascular diseases (CVDs) encompass disorders affecting the heart and blood vessels, including coronary artery disease, heart failure, hypertensive heart disease, cardiomyopathies, arrhythmias, congenital defects, and thromboembolic conditions. CVDs are the leading cause of death globally, accounting for the majority of mortality in both men and women. Given their substantial clinical and socioeconomic burden, research in cardiovascular biology, vascular inflammation, lipid metabolism, and thrombosis is critical for advancing preventive strategies, optimizing pharmacological interventions, and reducing long-term complications.

Azelaprag
AMG 986
T143902049980-18-7In house
Azelaprag (AMG 986) is an oral apelin receptor agonist (EC50 = 0.32 nM). Azelaprag may be used to treat neurological disorders, cardiovascular diseases, and obesity with metabolic syndrome.
  • $107
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5-HT2 antagonist 1
T12597191592-09-3In house
5-HT2 antagonist 1 is a small molecule antagonist functioning as a 5-HT2B receptor antagonist (IC50 = 33.4 nM), with oral bioactivity and weak inhibition of α1 receptors, employed in research on hepatocellular carcinoma and related diseases.
  • $714
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TargetMol | Inhibitor Hot
Resiniferatoxin
RTX, [3H]resiniferatoxin
T3429557444-62-9
Resiniferatoxin ((+)-Resiniferatoxin) is a highly potent synthetic TRPV1 agonist that inhibits the production of Th1 cytokines and has anti-inflammatory activity, reducing serum levels of IL-12, INF-γ, IL-1β, TNF-α, NO, and PGE.
  • $456
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TargetMol | Inhibitor Hot
Tirzepatide
LY-3298176
TP11112023788-19-2
Tirzepatide (LY-3298176) is a dual agonist of glucose-dependent polypeptide (GIP) (EC50=0.042 nM) and glucagon-like peptide-1 (GLP-1) (EC50=0.086 nM) receptors, and it has neuroprotective activity. It can improve blood pressure and lower low-density lipoprotein (LDL) cholesterol and triglycerides, and can be used to study diabetes and obesity.
  • $266
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TargetMol | Inhibitor Hot
AZD0780
PCSK9-IN-12, EX-A6975
T643622455427-91-3
AZD0780 (EX-A6975, PCSK9-IN-12) is an orally active PCSK9 inhibitor with high affinity for PCSK9 (Kd < 200 nM). It binds to a specific pocket in the C-terminal domain of PCSK9 without affecting the PCSK9–LDLR interaction. AZD0780 blocks the lysosomal trafficking of the PCSK9–LDLR complex and prevents PCSK9-induced LDLR degradation, making it useful for studies related to hypercholesterolemia.
  • $66
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TargetMol | Inhibitor Hot
Resmetirom
VIA-3196, MGL3196
T3595920509-32-6
Resmetirom (MGL-3196) is a THR-β agonist (EC50=0.21 μM), with high selectivity and oral activity. Resmetirom can be used in the research of non-cirrhotic and non-alcoholic steatohepatitis.
  • $33
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TargetMol | Inhibitor Hot
TargetMol | Citations Cited
Ruxolitinib
INCB018424, (R)-Ruxolitinib
T1829941678-49-5
Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
  • $53
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TargetMol | Inhibitor Hot
TargetMol | Citations Cited
AZD5462
T638382787501-83-9
AZD5462 is a potent orally available relaxin receptor RXFP1 agonist for the study of heart failure and cancer.
  • $289
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TargetMol | Inhibitor Hot
GSK484 hydrochloride
GTPL8577, AOB6992
TQ00671652591-81-5
GSK484 hydrochloride (GTPL8577) is a reversible peptidyl-arginine deiminase 4 (PAD4) inhibitor. It binds to PAD4 with high affinity, with IC50 of 250 and 50 nM in the presence and absence of 2 mM calcium, respectively. GSK484 promotes the radiosensitivity of colorectal cancer (CRC) and inhibits NET formation in vitro and in vivo.
  • $65
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TargetMol | Inhibitor Hot
TargetMol | Citations Cited
D-GsMTx4 TFA
T37697L
D-GsMTx4 TFA belongs to natural products and is a TRPC1/6 and Piezo2 channel inhibitor with high selectivity and cell permeability, inhibiting Ca2+ influx and the mTOR pathway. This compound is used in research on myocardial infarction, chronic pain, and pulmonary fibrosis.
  • $163
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TargetMol | Inhibitor Hot
CNS-5161 hydrochloride
CNS 5161A
T10852160756-38-7In house
CNS-5161 hydrochloride (CNS 5161A) is a small molecule antagonist and an NMDA receptor antagonist that selectively and non-competitively blocks the action of glutamate, and can be used for research on neurological diseases.
  • $509
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Ceruletide
FI-6934, Cerulein, Caerulein
T1493217650-98-5
Ceruletide is a decapeptide that serves as a safe and effective cholecystokinin receptor agonist, exerting a direct spasmogenic effect on the gallbladder muscle and bile ducts, and is commonly used to establish pancreatitis models.
  • $31
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TargetMol | Citations Cited
Evolocumab
T99201256937-27-5
Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.
  • $228
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TargetMol | Inhibitor Hot
KDM4-IN-4
T603542230475-63-3In house
KDM4-IN-4 is a histone lysine demethylase 4 (KDM4) inhibitor that primarily targets the Tudor domain of KDM4A and exhibits anticancer activity. KDM4-IN-4 has an affinity for the KDM4A Tudor domain of approximately 80 μM. KDM4-IN-4 inhibits the binding of H3K4Me3 to the Tudor domain in cells, with an EC50 of 105 μM. KDM4-IN-4 can be used in cancer research.
  • $293
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Candoxatril
UK 79300
T10671123122-55-4In house
Candoxatril (UK 79300) is a small-molecule inhibitor and a neutral endopeptidase (NEP) inhibitor with oral activity and cell permeability, used for the treatment of chronic heart failure and capable of improving exercise capacity in patients receiving angiotensin-converting enzyme inhibitor therapy.
  • $293
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TargetMol | Inhibitor Hot
LDL-IN-3
T10063180908-67-2In house
LDL-IN-3 belongs to synthetic compounds and is an antioxidant and anti-atherosclerotic agent with good cell permeability and cardiovascular protective properties. This compound is used for the treatment of atherosclerosis-related diseases, effectively inhibiting oxidative stress and lipid deposition, and reducing arterial plaque formation.
  • $388
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Alirocumab
T99161245916-14-6
Alirocumab is a human monoclonal antibody that inhibits PCSK9. It is produced by recombinant DNA technology in Chinese hamster ovary cell suspension culture.
  • $247
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TargetMol | Inhibitor Hot
VBIT-4
T132872086257-77-2
VBIT-4 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 17 μM). VBIT-4 can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).
  • $68
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TargetMol | Citations Cited
Yoda 1
T7506448947-81-7
Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1/26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).
  • $39
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TargetMol | Citations Cited
Galunisertib
LY2157299
T2510700874-72-2
Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.
  • $40
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TargetMol | Citations Cited
Abelacimab
MAA868, MAA 868
T768942098724-83-3
Abelacimab (MAA868), a fully human IgG1 monoclonal antibody that binds to and blocks the activation of FXI, is an anticoagulant used in the study of thromboembolic diseases.
  • $228
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Ecastolol
T1114877695-52-4In house
Ecastolol is a small molecule inhibitor, a β-adrenergic receptor antagonist that exerts its pharmacological effect by blocking catecholamine-induced agonism of this receptor, with anti-anginal properties, used for cardiovascular disease research.
  • $388
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Finerenone
BAY94-8862, BAY-94-8862, BAY-948862, BAY948862, BAY 94-8862, BAY 948862
T213951050477-31-0
Finerenone (BAY-948862) is a nonsteroidal antagonist of the mineralocorticoid receptor (MR) (IC50=18 nM) with selective and oral activity. Finerenone is used in the treatment of patients with chronic kidney disease with type 2 diabetes.
  • $31
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TargetMol | Inhibitor Hot
TargetMol | Citations Cited
Metformin
1,1-Dimethylbiguanide
T8526657-24-9
Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.
  • $39
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TargetMol | Inhibitor Hot
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