CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a selective modifier of the gap junction protein.
ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.IC50 value: 19 nM (rat Nav1.7) [1]Target: rat Nav1.7 inhibitorICA-121431 exhibited a spectrum of inhibitory activity for Nav human channel subtypes; equipotent inhibition of Nav1.3 and Nav1.1, less potent inhibition of Nav1.2, and much weaker inhibition of Nav1.7, Nav1.6, Nav1.4, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM). the unique subtype selective Nav channel inhibitors ICA-121431 and PF-04856264 interact with amino acid residues on an extracellular facing region of the homologous Domain 4 voltage sensor of Nav1.3 or Nav1.7, which is distinct from previously described interaction sites for TTX or local anesthetic-like Nav channel inhibitors.
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Palmitic acid-d2 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
ICI141292 is a potent β-adrenoceptor partial agonist with a greater affinity for β1- than β2-adrenoceptors.
Ganoderic acid K is a potent angiotensin converting enzyme inhibitor. Ganoderic acid K is a triterpene that can be found in ganoderma lucidum[1].
PAMP-12(human, porcine) is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control[1].
Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside[1]. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years[2].
Fesomersen (sodium) is an antisense oligonucleotide designed to inhibit the production of Factor XI.
Milrinone lactate is a potent inotropic dilating agent. Milrinone lactate shows simultaneous positive inotropic and vasodilating activities. Milrinone lactate promotes reduction of SVR and PVR in patients with DCM and NYHA class III and IV of heart failure. Milrinone lactate has the potential for the research of cardiovascular function after cardiac surgery and in septic shock[1][2].
GW3965 hydrochloride is a potent and selective LXR agonist with EC50s of 190 and 30 nM for hLXRα and hLXRβ , respectively.
Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation[1][2].
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes[1].
Rivaroxaban is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
WNK-IN-11 D3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11 D3 is effective at regulating cardiovascular homeostasis[1].
U-89232 appears to be a cardioselective KATP channel opener.
Palonidipine is a calcium antagonist which is potential for the therapy of angina-pectoris and hypertension[1][2][3].
Bemoradan (compound 10a) is an orally active and selective canine Phosphodiesterase (PDE) fraction III inhibitor. Bemoradan is a long-acting, potent, inotropic vasodilator and a novel cardiotonic agent, and can be used in congestive heart failure research[1].
L-Aspartic acid-d3,15N is the deuterium and 15N-labeled L-Aspartic acid. L-Aspartic acid is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities[1][2].
Bradykinin (1-6) is an amino-truncated Bradykinin peptide. Bradykinin (1-6) is a stable metabolite of Bradykinin, cleaved by carboxypeptidase Y (CPY).
Pelacarsen (AKCEA-APO(a)-LRx) is a liver-specific antisense oligonucleotide against apolipoprotein(a) that reduces lipoprotein(a) up to 80% with good tolerability[1].
Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with IC50 of 1.5 nM.
GRK2 Inhibitor 2 (Compound 8h) is a GRK2 inhibitor (IC50: 19 nM). GRK2 Inhibitor 2 also inhibits Aurora-A (IC50: 137 nM). GRK2 Inhibitor 2 promotes β-AR-mediated cAMP accumulation in GRK2-overexpressed HEK293 cells. GRK2 Inhibitor 2 can be used for research of congestive heart failure (HF)[1].
Mant-GTPγS, a GTP mimetic, is a potent competitive adenylyl cyclase (AC) inhibitor. Mant-GTPγS is a potent YdeH inhibitor[1][2][3].
Butalamine is a vasodilator[1].
Thio-ITP (6-Thioinosine 5′-triphosphate) is a RNA polymerase activities competitive inhibitor[1].
Molsidomine is an orally active, long acting vasodilating drug, metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gαq and βarr2 response, with pEC50 values of 8.31 and 8.44, respectively[1].