Flavanomarein is a predominant flavonoid of Coreopsis tinctoria Nutt with protective effects against diabetic nephropathy. Flavanomarein has good antioxidative, antidiabetic, antihypertensive and anti-hyperlipidemic activities[1][2].
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251, is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm)[1][2].
ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).IC50 value: 4 nM/16 nM(thallium influx fluorescent assay/automated electrophysiology assay) [1]Target: KCNK3 blockerML365 possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.
Bradykinin (1-3) is a 3-amino acid residue peptide. Bradykinin (1-3) is an amino-truncated Bradykinin peptide, cleaved by Prolyl endopeptidase.
Alisol C 23-acetate, a natural product extracted from Alisma orientale, can significantly and strongly inhibit DTH response after oral administration.
Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Efaroxan hydrochloride is a potent and selective α2-adrenoceptor antagonist, antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist and can be used for the research of cardiovascular disease[1][2][3].
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is ＞25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively[1].
Ladanetin-6-O-β-D-glucopyranoside is an active flavonoid. Ladanetin-6-O-β-D-glucopyranoside has antioxidative effect. Ladanetin-6-O-β-D-glucopyranoside can be used for the research of cardioprotective effects[1].
TT-10 (YAP-TEAD activator TT-10) is a small molecule activator that activates pro-proliferative YES-associated protein (YAP) and transcriptional enhancer factor domain (TEAD) activities in cardiomyocytes; promoted cardiomyocyte proliferation and simultaneously exerted antioxidant and antiapoptotic effects in vitro via nuclear translocation of YAP, activates YAP-TEADs activity and the Wnt/β-Catenin signaling pathway; ameliorates cardiac dysfunction, decreases ROS and DNA aamage and apoptosis after myocardial infarction (MI) in mice.
Denudatine, is primarily isolated from plants of the genera Aconitum and Delphinium[1]. Denudatine has effects on action potential of ventricular fibers and inhibits arrhythmogenic action of aconitine[2].
Neladenoson dalanate is a potent, selective, orally acitve partial adenosine A1 receptor (A1AR) agonist (EC50=0.1 nM) for the treatment of chronic heart failure. Heart Failure Phase 2 Clinical
Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation[1].
Clopidogrel sulfate is an antiplatelet agent. Specifically, Clopidogrel sulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. Clopidogrel sulfate can be used for research of heart disease and stroke[1].
Atropine is a medication used to treat certain types of nerve agent and pesticide poisonings, some types of slow heart rate, and to decrease saliva production during surgery.
PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe2+ ion and induces the formation of an “Arg367-out” pocket[1].
Nordefrin ((±)-Cobefri), a Norepinephrine derivative, is a vasoconstrictor agent[1].
Phentolamine mesylate is a competitive, reversible α-adrenoceptor antagonist with an IC50 between 5 and 30 nM.
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controlling acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock treatment[1][2][3][4][5].
Valsartan (CGP-48933) is an angiotensin II receptor antagonist for treatment of high blood pressure and heart failure.
Phosphorylcholine is an antigenic cell-surface component found on many commensal and pathogenic bacteria that reside in the upper airway.
Nilvadipine is a potent calcium channel antagonist, and the IC50 value is around 0.1 nM.
CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC50 of 2.9 μM. CDK2-IN-15 can be used for cancer research[1].
N-acetyl lysyltyrosylcysteine amide (KYC) is a potent, tripeptide inhibitor of myeloperoxidase (MPO), inhibits MPO-mediated hypochlorous acid (HOCl) formation (IC50=7 uM) and nitration/oxidation of LDL; completely inhibits HOCl production at 25 uM, decreases vascular oxidative stress and increases vasodilatation in sickle cell disease mice; reduces oxidative stress-mediated inflammation, neuronal damage, and neural stem cell injury in murine model of stroke.
GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity[1][2][3].
Pravastatin is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.Target: HMG-CoA reductasePravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used in combination with diet, exercise, and weight-loss for lowering cholesterol and preventing cardiovascular disease.Pravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.The evidence for the use of pravastatin is generally weaker than for other statins. The antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT), failed to demonstrate a difference in all-cause mortality or nonfatal myocardial infarction/fatal coronary heart disease rates between patients receiving pravastatin 40mg daily (a common starting dose) and those receiving usual care.
Digoxin is a potent inhibitor of Na+/K+-ATPase, clinically used to treat arrhythmia and heart failure.
Ornipressin is a potent vasoconstrictor, hemostatic and renal agent. Sequence: Cys-Tyr-Phe-Gln-Asn-Cys-Pro-{Orn}-Gly-NH2 (Disulfide bridge: Cys1-Cys6).