Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K+ current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent[1].
Lomitapide mesylate(AEGR-733; BMS-201038) is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM.IC50 value: 8 nM [1]Target: MTP inhibitorLomitapide is a small-molecule, microsomal triglyceride transfer protein (MTP) inhibitor, for the treatment of both familial and primary hypercholesterolemia. Oral, once-daily lomitapide will be targeted at patients resistant to HMG-CoA reductase inhibitors (statins) either due to abnormalities in liver function or to discontinuation because of muscle pain.
Breviscapine is a crude flavonoid extract of Breviscapine, which is more than 85% of the active ingredient, Breviscapine. Breviscapine has a wide range of cardiovascular pharmacological activities, such as increasing blood flow, improving microcirculation, dilating blood vessels, reducing blood viscosity, promoting fibrinolysis, inhibiting platelet aggregation and thrombosis. Breviscapine has been used in the study of cerebral infarction and its sequelae, cerebral thrombosis, coronary heart disease and angina pectoris[1][2].
KR-32568 is a sodium/hydrogen exchanger-1 (NHE-1) inhibitor with an IC50 of 230 nM. KR-32568 has cardioprotective effects[1][2].
Angiogenin (108-122) is an angiogenin peptide.
Brain Natriuretic Peptide-45, mouse (BNP-45, mouse) is a circulating form of mouse brain natriuretic peptide isolated from mouse heart with potent hypotensive and natriuretic potency[1][2].
SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway[1][2][3].
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration[1][2][3].
Anti-MI/R injury agent 1 (compound 18), a Panaxatriol derivative, is an orally active, potent anti-myocardial ischemia/reperfusion (anti-MI/R) injury agent. Anti-MI/R injury agent 1 enhances oxygen-glucose deprivation and reperfusion (OGD/R)-induced cardiomyocyte injury cell viability. Anti-MI/R injury agent 1 can markedly reduce myocardial infarction size, decrease circulating cardiac troponin I (cTnI) leakage, and alleviate cardiac tissue damage in the rats[1].
Trombodipine is an antithrombotic agent.
ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective Nox1 inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.
Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide. Big Endothelin-1 (1-39), porcine has similar pressor effects in vivo[1].
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure[1].
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
Ep vinyl quinidine (3-Epiquinine) is an epi-vinyl stereoisomer of Quinidine. Quinidine is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine can be used for malaria research[1][2][3].
TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC50 of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent[1].
Vitexin-4''-O-glucoside is a kind of flavonoid fraction from the leaves of Crataegus pinnatifida[1].
Bendazol is a hypotensive drug which can also enhance NO synthase activity in renal glomeruli and collecting tubules.
Proadrenomedullin (45-92), human, a mid-regional fragment of proadrenomedullin (MR-proADM), comprises amino acids 45–92 of pre-proADM. Proadrenomedullin (45-92), human has a longer half-life, is relatively stable and is produced in equimolar amounts to adrenomedullin (ADM), making it a surrogate for plasma levels of ADM gene products[1][2].
3-Methylsalicylic acid is a salicylic acid derivative compound with marked fibrinolytic activity in human plasma by activating its fibrinolytic system.
Thromboxane B1 (TXB1) is one of thromboxane B (TXB) family members. Thromboxane is a member of the family of lipids known as eicosanoids. Thromboxane is named for its role in blood clot formation (thrombosis)[1].
Cimlanod is a second-generation nitroxyl (HNO) donor. Heart Failure Phase 2 Clinical
TDSRCVIGLYHPPLQVY is a disordered control peptide. TDSRCVIGLYHPPLQVY is a peptide containing the same amino acids as LP17 (HY-P3400) but in a different sequence order[1][2].
Xylometazoline Hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.Target: α-AdrenoceptorXylometazoline is a nasal decongestant spray that constricts nasal blood vessels and increases nasal airflow, enabling patients with a blocked nose to breathe more easily. Xylometazoline is an effective and well-tolerated decongestant nasal spray that significantly relieved nasal congestion compared with placebo in the common cold and provided long-lasting relief with just 1 spray, helping patients to breathe more easily for a longer period of time [1]. Xylometazoline exhibited in radioligand competition studies higher affinities than the catecholamines adrenaline and noradrenaline at most α-adrenoceptor subtypes. Xylometazoline behaved at α(2B) -adrenoceptors as full agonists [2].
Encainide (MJ9067) is an antiarrhythmic drug with class ⅠC activity. Encainide has the potential for life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias and supraventricular arrhythmias research[1].
Lercanidipine-13C,d3 (hydrochloride) is the deuterium and 13C labeled Lercanidipine hydrochloride[1]. Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[2][3][4].
Puliginurad (YL-90148) is a potent urate transporter (URAT) inhibitor. Puliginurad can be used for hyperuricemia and gout research[1].
Dexrazoxane(ICRF187) is a cardioprotective agent.Target: OthersDexrazoxane is a cardioprotective agent. Dexrazoxane is a derivative of EDTA, dexrazoxane chelates iron and thus reduces the number of metal ions complexed with anthracycline and, consequently, decrease the formation of superoxide radicals. The exact chelation mechanism is unknown, but it has be postulated that dexrazoxane can be converted into ring-opened form intracellularly and interfere with iron-mediated free radical generation that is in part thought to be responsible for anthryacycline induced cadiomyopathy. It was speculated that dexrazoxane could be used for further investigation to synthesize new antimalarial drugs [1, 2].
(S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity[1].