Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway[1].
Praeruptorin E is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2′ value of 5.2[1].
Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
Fosfructose trisodium (Diphosphofructose trisodium;Esafosfan trisodium;FDP trisodium) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.
Cadralazine (ISF 2469) is an orally active antihypertensive agent. Cadralazine is a peripheral arteriolar vasodilator[1].
Cinepazide Maleate is a vasodilator.Target: OthersCinepazide maleate is a maleate salt form of cinepazide which is a vasodilator. Cinepazide (30 mg/kg, i.v.) potentiated the vertebral vasodilator response of dogs to intravertebral adenosine and cyclic AMP, Intravertebral cinepazide(1-10 mg) increased vertebral blood flow in a dose-related manner and the effect was partially inhibited by intravenous pretreatment with aminophylline but not by pretreatment with autonomic antagonists. Cinepazide resembled cinnarizine and papaverine in that the drug antagonized rabbit aortic contraction induced by KCl, norepinephrine or CaCl2 [1]. Cinepazide in concentrations ranging from 10-6 to 10-5M augmented the relaxing responses to ATP, adenosine and cAMP. However, this agent did not affect the relaxations induced by isoproterenol and papaverine and the contractions induced by 5-HT, prostaglandin F2α and ATP. cinepazide selectively potentiates the relaxing response mediated through purinergic P1 receptors [2].
Squalene is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity.
DMTr-4'-Me-U-CED-TBDMS phosphoramidite (DMTr-4'-Methyluridine-CED-TBDMS phosphoramidite), a dye reagent for oligonucleotide labeling, can be used for the research of applications in RNA therapeutics, RNA aptamers, and ribozymes for elucidating RNA structure. DMTr-4'-Me-U-CED-TBDMS phosphoramidite represents a probe with wide utility for elucidation of RNA structure[1].
Olpasiran is a small interfering RNA that reduces lipoprotein(a) synthesis in the liver.
Istaroxime hydrochloride is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM.
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects[1].
Cetaben, an exceptional type of peroxisome proliferator, is a peroxisome proliferator-activated receptor α (PPARα)-independent peroxisome proliferator. Cetaben is a non-fibrate hypolipidemic drug and potently reduces the concentration of cholesterol and triglycerides[1][2].
PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis[1].
APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively[1].
PI3KC2α-IN-2 is a potent and selective PI3KC2α inhibitor (IC50: 121 nM). PI3KC2α-IN-2 interacts with the ATP-binding site of PI3KC2α.. PI3KC2α-IN-2 can be used in the research of thrombosis, diabetes and cancers[1].
Piridoxilate (Piridoxylate), a glyoxylate derivative, is an anti-anoxic agent. Piridoxilate can be used in research on vascular diseases and coronary occlusion[1][2].
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.IC50 value: Target: HERG activatorRPR260243 displayed no activator-like effects on other voltage-dependent ion channels, including the closely related erg3 K+ channel. RPR260243 enhanced the delayed rectifier current in guinea pig myocytes but, when administered alone, had little effect on action potential parameters in these cells. However, RPR260243 completely reversed the action potential-prolonging effects of dofetilide in this preparation. Using the Langendorff heart method, we found that 5 μM RPR260243 increased T-wave amplitude, prolonged the PR interval, and shortened the QT interval. We believe RPR260243 represents the first known HERG channel activator and that the drug works primarily by inhibiting channel closure, leading to a persistent HERG channel current upon repolarization.
Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research[1].
Fosinopril-d5 sodium (SQ28555-d5 sodium) is the deuterium labeled Fosinopril sodium. Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure[1][2].
Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.
Theodrenaline hydrochloride is a cardiac stimulant, also acts as an anti-hypotensive agent together with Cafedrine.
Ritivixibat is an inhibitor of ileal bile acid transporter (IBAT), as well as a bile acid modulator. Ritivixibat can be used for research of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases[1][2].
Picotamide is a combined inhibitor of thromboxane A2 (TxA2) synthase and receptor. Picotamide has antiplatelet activity. Picotamide promotes the reduction of microalbuminuria and the inhibition of growth of carotid plaques in diabetes. Picotamide can be used for researching acute or chronic cardiovascular diseases[1].
Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with natriuretic/diuretic properties. Fenoldopam stimulated cAMP accumulation in LLC-PK1 cells in a dose-dependent manner, an effect which could be blocked by the DA1-selective antagonist Sch 23390. Although fenoldopam was more potent than DA (EC50 55.5 +/- 7.75 nM vs. 1.65 +/- 0.64 microM) in stimulating cAMP accumulation in LLC-PK1 cells, the maximum stimulation obtained by fenoldopam was only 37% of the maximum stimulation obtained by DA(Emax 13.0 +/- 2.95 pmol/mg of protein vs. 35.6 +/- 10.19 pmol/mg of protein) [1]. Fenoldopam is a selective dopamine1 (DA1) receptor agonist. Most of the DA1 receptor agonist activity of fenoldopam resides in the R-enantiomer, which also shows weaker alpha 2-adrenoceptor antagonist activity Fenoldopam produces vasodilation in vascular beds that are rich in vascular DA1 receptors [2].
GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.IC50 value: 27 pMTarget: sEHin vitro: GSK2256294A also displays potent cellular inhibition (IC50 = 0.66 nM) of sEH in an assay developed using a cell line transfected with the human sEH enzyme. [1]in vivo: A novel, potent, selective inhibitor of recombinant human, rat and mouse sEH, GSK2256294A, exhibits potent cell-based activity, a concentration-dependent inhibition of the conversion of 14,15-EET to 14,15-DHET in human, rat and mouse whole blood, and a dose-dependent increase in the LTX/LTX diol ratio in rat plasma following oral administration. Mice receiving 10 days of cigarette smoke exposure concomitant with oral administration of GSK2256294A exhibits significant, dose-dependent reductions in pulmonary leukocytes and keratinocyte chemoattractant levels. Mice receiving oral administration of GSK2256294A following 10 days of cigarette smoke exposure exhibited significant reductions in pulmonary leukocytes compared to vehicle-treated mice.
Norswertianolin acts as a CSE activator and is isolated from G. acuta. Norswertianolin may be a potential agent for cardiovascular diseases[1][2].
Anemarrhenasaponin A2 (Schidigerasaponin F2;Timosaponin AII) is a steroidal saponin isolated from the rhizomes of Anemarrhena asphodeloides. Anemarrhenasaponin A2 inhibits ADP-induced platelet aggregation[1].
Methyl 4-iodo-L-phenylalaninate hydrochloride is a Phenylalaninate derivative. Methyl 4-iodo-L-phenylalaninate hydrochloride can be used for the preparation of factor XI modulators used in the research of thrombotic and thromboembolic. Methyl 4-iodo-L-phenylalaninate hydrochloride can also be used for the synthesis of compounds for the research of amyloid-related diseases, such as Alzheimer’s disease[1][2].
VBIT-4 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (Kd) of 17 μM. VBIT-4, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases[1].