Curcumenone is a major constituent of the plants of medicinally important genus of Curcuma. Curcumenone, a caraborane type sesquiterpene has been reported to be a vasorelaxant, hepatoprotective and an effective inhibitor of intoxication[1].
DCN1-UBC12-IN-3 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.25 nM. Anticardiac fibrotic effect[1].
IM-54 is a selective inhibitor of oxidative stress-induced necrosis. IM-54 shows potent inhibitory activity against H2O2-induced necrosis. IM-54 acts as a potential cardioprotective agent and biological tool for investigating the molecular mechanisms of cell death[1][2].
Pratosartan is a selective angiotensin II receptor antagonist.
Centhaquine (Centhaquin; PMZ-2010) is a novel agent has the potential for treatment of haemorrhagic shock. Centhaquine (Centhaquin; PMZ-2010) can augment cardiac output, reduce systemic vascular resistance in haemorrhagic models[1][2].
A81988 is a potent, competitive, non-peptidic antagonist of angiotensin AT1 receptors.
Homoeriodictyol 7-O-β-D-glucoside is a natural platelet-activating factor (PAF) antagonist. Homoeriodictyol 7-O-β-D-glucoside inhibits human and rabbit platelet aggregation induced by PAF, with an IC50 of 0.8 μM[1].
KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and 5050s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.
Propafenone Hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.Target: Sodium ChannelPropafenone Hydrochloride is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias. According to the Allergic Rhinitis and its Impact on Asthma (ARIA) treatment guidelines, intranasal anti-histamines are recommended for the first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis (new classification system for rhinitis). Propafenone works by slowing the influx of sodium ions into the cardiac muscle cells, causing a decrease in excitability of the cells. Propafenone is more selective for cells with a high rate, but also blocks normal cells more than class Ia or Ib. Propafenone differs from the prototypical class Ic antiarrhythmic in that it has additional activity as a beta-adrenergic blocker which can cause bradycardia and bronchospasm .
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. CRTh2 antagonist 3 (compound 4) also enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation[2].
Cartilostatin 1 is an anti-angiogenic peptide. Cartilostatin 1 can be used for the research of anti-angiogenic[1].
Resveratroloside is a competitive inhibitior of α-glucosidase with an IC50 of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect[1][2].
Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.ic50 value: 50 μMTarget: PAFin vitro: Aglafoline also inhibits [3H]PAF (3.6 nM) binding to washed rabbit platelets with an IC50 value of 17.8 ± 2.6 μM. The concentration-response curve of PAF-induced platelet aggregation was shifted to the right by Aglafoline with pA2 and pA10 values of 5.97 and 5.04, respectively. Although thromboxane B2 formation caused by collagen and thrombin was partially suppressed by Aglafoline, thromboxane B2 formation caused by ionophore A23187 and arachidonic acid was not affected. Aglafoline inhibited the [3H]inositol monophosphate formation caused by PAF but not that caused by collagen or thrombin in the presence of indomethacin (20 μM). [1]in vivo: The cAMP content of washed rabbit platelets was not affected by Aglafoline. Rat femoral intravenous administration of Aglafoline (10 mg/kg) did not affect blood pressure. However, Aglafoline (10 mg/kg) both prophylactically and therapeutically antagonized PAF (2.5 μg/kg)-induced hypotensive shock in rats. Intravenous PAF (30 ng/kg) caused severe bronchoconstriction in guinea pigs. This effect was completely blocked by Aglafoline. This implies Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo.[1]
Scospondistatin is an anti-angiogenic peptide that can inhibit proliferation and migration of human umbilical vein endothelial cells in vitro[1].
Angiotensinogen (1-14), human is a fragment of the renin substrate angiotensinogen, a precursor for all angiotensin peptides.
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na+/K+-ATPase whereas in microsomes, both Na+/K+-ATPase and Mg2+-ATPase activities are significantly stimulated in a dose-dependent manner[1]. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells[2].
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes[1][2][3].
S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ[1].
Fosfructose is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma.
DRP1i27 is a potent inhibitor of human Drp1 (dynamin-related protein 1). DRP1i27 binds to the GTPase site of Drp1, with hydrogen bonds to Gln34 and Asp218. DRP1i27 targets Drp1-mediated mitochondrial fission in cell line models and protects against simulated ischemia-reperfusion injury[1].
CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM[1].
Glisoxepid-d4 is the deuterium labeled Glisoxepide. Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect[1][2][3].
Phenoxybenzamine hydrochloride is a selective antagonist of both α-adrenoceptor and calmodulin that is commonly used for the treatment of hypertension, specifically caused by pheochromocytoma.
Hirullin P18 is a potent thrombin inhibitor. Hirullin P18 has an anticoagulant effect[1].
Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.
Rubiayannone A is an anthraquinone glycoside with an antiplatelet aggregation activity[1].
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.
Prolylleucine is a dipeptide containing branched-chain amino acids.
Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.IC50 value: 1.5 nM [1]Target: reninin vitro: Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans [2].in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4].