Imidapril Hydrochloride is the hydrochloride salt of Imidapril, an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Target: ACEAs a prodrug, Imidapril is converted by hydrolysis in the liver into its active form imidaprilat. Imidaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Imidaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.
Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate[1][2].
CTP is a cardiac targeting peptide. CTP transduces cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be used to deliver therapeutic peptides, proteins and nucleic acid specifically to the heart[1].
A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.
Maritimein is an aurone that can be isolated from Coreopsis tinctoria. Maritimein shows strong diphenyl(2,4,6-trinitrophenyl)iminoazanium (DPPH) radical-scavenging activity with an IC50 value of 4.12 μM. Maritimein can be used for the research of cardiovascular disease[1].
3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study[1].
Nicotinic acid N-oxide is used to treat hyperlipoidemia.
ITD-1 is the first selective TGFβ inhibitor with an IC50 of 460 nM.
NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research[1].
Bometolol Hydrochloride is a beta-adrenergic blocking agent, used for the research of cardiovascular disease.
Jesaconitine is a toxic alkaloid. Jesaconitine can be derived from Aconitum. Jesaconitine is one of the major metabolites that can be detected in the blood of the right atrium after aconitum poisoning. Various types of arrhythimia are characteristic in aconitine intoxication[1].
Sar-Pro-Arg-pNA is a chromogenic substrate of α-thrombin. Sar-Pro-Arg-pNA can be used to test α-thrombin activity[1].
E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.IC50 value:Target: K+ channel blockerin vitro: Dofetilide and E-4031 induced EADs or TdP in all assays (50-83%), and the induction correlated with a significant increase in beat-to-beat variability of repolarization [1]. E-4031 (0.1 mumol/L) significantly prolonged cycle length and action potential duration, depolarized maximum diastolic potential, and reduced both the upstroke velocity of the action potential and the diastolic depolarization rate [2].in vivo: E-4031 in doses of 0.01 and 0.1 mg/kg that can provide the plasma concentrations effectively to inhibit IKrin vitro significantly delayed the repolarization beyond the initiation of diastole, resulting in the inversion of electro-mechanical coupling, which provides an ideal proarrhythmic substrate, while the durations of left ventricular systole and diastole remained the same [3]. Bepridil and E-4031 prolonged QT interval and ARI in all LV layers, though the magnitude of prolongation was greatest in Mid, increasing the transmural ARI dispersion, particularly during bradycardia [4].
Bradykinin (1-7) is an amino-truncated Bradykinin peptide. Bradykinin (1-7) is a metabolite of Bradykinin, cleaved by endopeptidase.
L 640035 is athromboxaneantagonist[1].
Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties[1].
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure[1][4].
COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks[1].
Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension[1][2].
Eprosartan is a nonpeptide angiotensin II receptor antagonist with IC50 of 9.2 and 3.9 nM in rat and human adrenal cortical membranes, respectively. IC50 Value: 9.2 nM(in rat adrenal cortical membranes); 3.9 nM(in human adrenal cortical membranes)Target: Angiotensin Receptor Type-1(AT1)in vitro: Eprosartan mesylate, is one of the highly selective, orally active, non-peptide angiotensin-II-receptor antagonists [1]. In rat and human adrenal cortical membranes, Eprosartan displaced specifically bound [125I]AII with IC50 of 9.2 and 3.9 nM, respectively. Eprosartan also inhibited [125I]AII binding to human liver membranes (IC50 = 1.7 nM) and to rat mesenteric artery membranes (IC50 = 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca++ levels. In rabbit aortic rings [2].in vivo: Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr. In this same rat model, Eprosartan had no effect on base-line pressure or on the pressor response to norepinephrine or vasopressin [2]. Eprosartan is highly effective and safe in lowering blood pressure, notably SBP, in older subjects with mild to moderate hypertension [3]. Treatment with eprosartan in once-daily doses up to 1200 mg alone or in combination with HCTZ was well tolerated, with dizziness and asthenia being the most common side effects [4]. Therapy with eprosartan mesilat was associated with significant hypotensive effect (more evident in patients with high systolic blood pressure), improvement in 24-hour blood pressure profile and quality of life, and lower probability of secondary stroke. Side effects were not observed [5].
α-Tocopherol phosphate (alpha-Tocopherol phosphate) disodium, a promising antioxidant, can protect against long-wave UVA1 induced cell death and scavenge UVA1 induced ROS in a skin cell model. α-Tocopherol phosphate disodium possesses therapeutic potential in the inhibition of apoptosis and increases the migratory capacity of endothelial progenitor cells under high-glucose/hypoxic conditions and promotes angiogenesis[1][2].
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy[1].
SL910102 is a nonpeptide angiotensin AT1 receptor antagonist.
Clonidine-d4 is the deuterium labeled Clonidine. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent[1][2][3][4][5].
Rac1-IN-3 (Compound 2) is a Rac1 inhibitor with an IC50 of 46.1 μM[1].
RXFP1 receptor agonist-1 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-1 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 300 nM[1].
Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is a hirugen-like peptide, and has high affnity for thrombin than Hirugen, with a KD < 100 nM. Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is an antithrombotic agent. Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) inhibits the thrombin-induced fibrin clot formation with an IC50 value of 0.087 μM[1].
Notoginsenoside FP2, a dammarane-Type Bisdesmoside isolated from the Fruit Pedicels of Panax notoginseng, has potential to treat cardiovascular disease[1][2].
Perhexiline maleate is a potent carnitine palmitoyltransferase 1 (CPT 1) inhibitor with IC50s of 77 and 148 μM for rat heart and liver CPT 1, respectively.