Fluvastatin sodium is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), used to treat hypercholesterolemia and to prevent cardiovascular disease.Target: HMGCR Fluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Human hepatocellular carcinoma cell (HCC) studies indicate that Fluvastatin induces G2/M phase arrest. In the presence of Fluvastatin, HCC cells show a decrease of Bcl-2 and procaspase-9 expression, and an increase in Bax, cleaved caspase-3, and cytochrome c. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].
12E,14-Trien-19-oic acid is a diterpenoid. 12E,14-Trien-19-oic acid can be isolated from Bhutanese medicinal plant, shug chher. 12E,14-Trien-19-oic acid can be used for the research of platelet aggregation[1].
Dechloro Rivaroxaban is a highly selective, orally active inhibitor of Factor Xa. Dechloro Rivaroxaban inhibits human free FXa with a Ki of 0.4 nM. Dechloro Rivaroxaban inhibits prothrombinase activity and fibrin-associated FXa activity with IC50s of 2.1 nM and 92 nM, respectively[1].
PF-1355 is a selective 2-thiouracil mechanism-based MPO inhibitor, used for treatment of vasculitic diseases.
Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
3-Methylchromone is an active compound which can be used in the prevention and research of anginose attacks of coronary origin[1].
Isomartynoside is a potent angiotensin converting enzyme (ACE) inhibitor with an IC50 value of 505.9 µM. Isomartynoside is a phenylpropanoid glycoside that can be found in Galeopsis pubescens[1][2].IC50: 505.9 µM (ACE)[1]
Bemfivastatin (PPD 10558) is an orally active, HMG-CoA Reductase (HMGCR) inhibitor, also known as Statin. Bemfivastatin enhances the activity of liver extraction. Bemfivastatin exhibits little developmental toxicity effects in pregnant rats and rabbits via daily oral doses during organogenesis period. The no observed adverse effect level (NOAEL) are ≥320 mg/kg/day for rats developmental toxicity, 12.5 mg/kg/day for rabbits maternal toxicity, and 25 mg/kg/day for rabbits developmental toxicity, respectively. Bemfivastatin can be used for research on Statin-related hypercholesterolemic myalgia with inability to tolerate statins[1][2].
Propafenone-d5 hydrochloride(Ethyl) (SA-79-d5 hydrochloride(Ethyl)) is the deuterium labeled Propafenone hydrochloride. Propafenone (SA-79）hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias[1].
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII)[1][2]. Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease[3].
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects[1][2][3].
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na+ transport produced by Alloxan[1][2]. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models[3].
Tetramethylpyrazine (Ligustrazine), an alkylpyrazine isolated from Ligusticum wallichii (Chuan Xiong)[1], is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Tetramethylpyrazine (Ligustrazine) also has potential nootropic and anti-inflammatory activities in rats[2][3].
BNP-45 (rat), a 45-amino acid brain natriurctic peptide isolated from rat heart, is a circulating hormone, with natriuretic andhypotensive activities.
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1].
FC9402 is a potent and selective sulfide quinone oxidoreductase (SQOR) inhibitor extracted from patent WO 2020/146636 A1. FC9402 attenuates TAC-induced cardiomyocyte hypertrophy and left ventricle (LV) fibrosis. FC9402 can be used for cardiovascular regulation[1].
C-Type Natriuretic Peptide (CNP) (1-22), human is the 1-22 fragment of C-Type Natriuretic Peptide. C-type natriuretic peptide is natriuretic peptide family peptide that is involved in the maintenance of electrolyte-fluid balance and vascular tone.
Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
Gepefrine is an orally active pressor agent and sympathomimetic agent. Gepefrine improves the early orthostatic disregulation of the arterial pressure[1][2][3].
Cicloprolol is a partial β 1-adrenoceptor agonist .
Epimedin K (Korepimedoside B), a flavonol glycoside, is isolated from the aerial parts of Epimedium koreanum Nakai. Epimedium koreanum Nakai is a famous Chinese herbal medicine for the research of impotence, osteoporosis, immune suppression and cardiovascular diseases[1][2].
YF-452 is a potential antiangiogenic drug candidate for cancer therapy.
Flavin Adenin Dinucleotide is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.
Ozagrel(OKY-046) is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.Target: Thromboxane A2 SynthaseOzagrel was selected as the best compound of highly selective inhibitors of TXA2 synthase. The inhibition of TXA2 synthase by ozagrel was more effective on human and rabbit enzymes than those of other species. Ozagrel increased 6-keto-PGF1 alpha, one of stable metabolites of PGI2, in various isolated cells and tissues perhaps via accumulated PG endoperoxides resulted by the inhibition of TXA2 synthase [1]. Ozagrel was estimated to be a reversible mixed-type inhibitor of diphenolase activity with the constants (K (S1), K (S2), K (i1), and K (i2)) determined to be 2.21, 3.89, 0.454, and 0.799 mM, repectively [2]. Infusion of OKY-046 significantly inhibited pulmonary thromboxane B2 delivery, attenuated the early increase in pulmonary vascular resistance, and blocked the increase in systemic vascular resistance. In addition, OKY-046 blunted and delayed the decrease in cardiac output and maintained end-systolic pressure-diameter relation, +dp/dt, and lung lymph flow at baseline values [3].
SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5[1].
HOKU-81, a new bronchodilator, is one of the metabolites of tulobuterol. IC50 Value: Target: Adrenergic ReceptorEffects of HOKU-81 on isolated trachea and atria of guinea pigs were compared with those of various bronchodilators. HOKU-81 appears to be a potent and selective beta 2-stimulant with a slight inotropic action. HOKU-81 was approximately 8 times more potent than tulobuterol, approximately twice as potent as salbutamol, and approximately as potent as isoprenaline in relaxing effect on the isolated tracheal smooth muscle preparation of guinea pigs. This effect of HOKU-81 seems to be due to direct action on the adrenergic beta-receptor.
Streptokinase is a bacteria-derived protein and a plasminogen activator. Streptokinase is widely used for the research of the blood-clotting disorders. Streptokinase improves reperfusion blood flow after coronary artery occlusion[1][2].
Pargyline hydrochloride is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension.
Teopranitol (KC-046), a coronary vasodilator with a rather selective venous dilatation, is used for the study of the acute myocardial ischemia[1].