(S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[2].
PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor with an IC50 of 3.96 µM. PCSK9-IN-20 decreases PCSK9 and increases LDLR protein expression in vitro[1].
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure[1].
5-Valine-angiotensin I is an Ang I peptide belonging to angiotensin I. 5-Valine-angiotensin I induces muscle contraction, can be used for renin-angiotensin system studies. Angiotensin I is a putative neurotransmitter, is the precursor of angiotensin II and of angiotensin fragment 1-7, which are involved in regulation of fluid volume and the release of aldosterone[1][2].
PD 113413 is formed by subsequent hydrolysis of the diketopiperazine quinapril analog. PD 113413 is a potent angiotensin-converting enzyme inhibitor. PD 113413 can be used for research of hypertension and congestive heart failure[1].
Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
Nitrendipine is a calcium channel blocker with marked vasodilator action.Target: Calcium ChannelNitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, when cells were held at hyperpolarized potentials, nitrendipine blocked Ca2+ currents much less potently (Kd approximately equal to 700 nM) [1, 2]. Nitrendipine, a potent analogue of nifedipine, binds in a reversible and saturable manner to partially purified guinea-pig heart membranes [3]. [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response [4].
MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.IC50 value: 1.65 μM (EC50, for hGPR109a), 1.08 μM (EC50, for mGPR109a) [1]Target: GPR109ain vitro: MK-0354 demonstrated clear and statistically significant partial agonism in the cAMP assays for both the mouse and human receptors with efficacy approximately 60-70% of that of either nicotinic acid or β-hydroxy butyrate, a putative physiologically relevant ligand for hGPR109a, in the same assay platform. In addition, MK-0354 showed no activation of GPR109b in the cAMP assay at any concentration up to 100 μM. Following these interesting observations, we then prepared a number of other 5,5-fused pyrazoles analogous to those that showed receptor activity in our earlier studies. MK-0354 appeared to be somewhat unique among the members of the pyrazole tetrazole series in having reasonable receptor activity.[1]in vivo: MK-0354 retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism, but did not induce vasodilation at the maximum feasible dose. Moreover, preadministration of MK-0354 blocked the flushing effect induced by nicotinic acid but not that induced by PGD2. This profile made MK-0354 a suitable candidate for further study for the treatment of dyslipidemia.[1] MK-0354 is a GPR109A partial agonist that activates the antilipolytic pathway in adipocytes. The single-dose and multiple-dose pharmacokinetics and pharmacodynamics, as well as tolerability, of MK-0354 were examined in two Phase I studies conducted in healthy male volunteers. The lipid efficacy of MK-0354 was assessed in a Phase II study conducted in male and female patients with dyslipidemia.[2]
(Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat (HY-139573). Etavopivat is an orally active erythrocyte pyruvate kinase-R (PKR) activator that can be used in studies of sickle cell disease and other haemoglobinopathies[1].
β-Hydroxypropiovanillone, a natural compound, shows significant concentration-dependent inhibitory effects on α-glucosidase with an IC50 of 257.8 μg/mL[1].
Acebutolol Hydrochloride is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.Target: β-Adrenergic ReceptorAcebutolol is a beta blocker for the treatment of hypertension and arrhythmias. Acebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9 mL/min/kg, the volume of distribution of 9.6 L/kg, and an elimination half-life of 1.8 hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5?mL/min/kg, the volume of distribution of 9.5?L/kg, and an elimination half-life of 2.3?hours [1]. Acebutolol (30 mg/kg) decreases cardiac output by 65% and 31% after 1 min and 10 min measurements, respectively, in Sprague-Dawley rats. Acebutolol (30 mg/kg) significantly reduces regional blood flow (RBF) in most organs either after 1 min or 10 min measurements when compare with the baseline values in Sprague-Dawley rats [2].
Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.Target: ACELisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Lisinopril may be used to treat hypertension and symptomatic congestive heart failure, to improve survival in certain individuals following myocardial infarction, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy [1, 2].
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.
Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity[1].
GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research[1].
Eburicoic acid protects the liver from CCl4-induced hepatic damage via antioxidant and anti-inflammatory mechanisms[1]. And Eburicoic acid has antidiabetic and antihyperlipidemic effects[2].
Fosfenopril is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes[1][2].
PF-184298 is a potent, selective dual serotonin and noradrenaline monoamine reuptake inhibitor (SNRI) with IC50 of 6 nM and 21 nM, respectively; displays good selectivity over dopamine reuptake inhibition (DRI) (IC50=544 nM); possesses good in vitro metabolic stability, weak CYP inhibition and drug-like physicochemical properties consistent with CNS target space.
D-Isofloridoside, one of the polysaccharide precursors, has the activity of scavenging free radicals, inhibiting ROS expression, and inhibiting MMP-2 and MMP-9[1][2].
ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively[1][2].
Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.IC50 value:Target: β1 receptor
Ethyl linoleate-13C18 (Linoleic Acid-13C18 ethyl ester) is the 13C labeled Ethyl linoleate. Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators[1].
Ciraparantag is a thrombin and factor Xa inhibitors as well as to heparin-based anticoagulants through non-covalent hydrogen bonding and charge interactions. It is reported to antagonize the effects of all coagulants except VKAs and agratroban. [1][2]
5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM[1].
FKK is an indazole derivative and also a novel bronchodilator.
Goflikicept (RPH 104) is a hybrid protein that selectively binds and inactivates both circulating IL-1ß and IL-1α. Goflikicept has the potential for the research of ST-segment elevation myocardial infarction (STEMI)[1].
Abelacimab (MAA868) is a fully human IgG1 monoclonal antibody that binds with high affinity to the catalytic structural domain of FXI and locks it in the zymogen conformation, thereby preventing its activation by FXIIa or thrombin. Abelacimab can be used in thromboembolic disease studies[1][2].
Antiarrhythmic agent-1 (example I) is an antiarrhythmic agent and an IKr potassium channel blocker (IC50<1 μM)[1].
HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively[1].
Ciraparantag TFA is a thrombin and factor Xa inhibitor. Ciraparantag TFA is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban[1][2][3][4].