SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty[1].
Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor[1][2][3].
(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease[1].
(R)-MLN-4760, the R-enantiomer of MLN-4760, is an ACE2 inhibitor, with an IC50 of 8.4 μM. (R)-MLN-4760 is the less active isomer[1].
MPO-IN-3 is a potent myeloperoxidase (MPO) inhibitor (WO2013068875A1, example 191). Myeloperoxidase (MPO) is a heme-containing enzyme belonging to the peroxidase superfamily[1].
Tafolecimab (IBI-306) is a human lgG2 monoclonal antibody that specifically binds PCSK-9 and reduces LDL-C levels by inhibiting PCSK-9-mediated endocytosis of the LDL receptor, which in turn enhances clearance of LDL-C and leads to a reduction in LDL-C levels. Tafolecimab may be used in studies of hypercholesterolaemia[1].
BI-1935 is a potent, selective small molecule inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 7 nM; BI-1935 is also highly active in a cellular Hep G2-DHET assay format with IC50 of <1 nM, BI-1935 can also be used in vivo and showed a dose dependent effect on mean arterial pressure blood pressure in Dahl salt sensitive rats; also shows good selectivity against hCYP epoxygenases 2J2/2C9/2C19 and IL-2.
PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).IC50 value: 0.26 ± 0.03 μM (Ki, for μ-calpain), 5.33 ± 0.77 μM (Ki, for m-calpain) [1]Target: calpainin vitro: The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity. [2]
UR-3216, a prodrug, is a selective and orally active platelet surface glycoprotein (GPIIb/IIIa) receptor antagonist. UR-3216 is the very tight binding of its active metabolite to platelets (Ki for resting platelets is < 1 nM). UR-2992, the active form of UR-3216, binds to platelets for a long period of time, while the unbound drug is rapidly cleared.
Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator[1][2].
YS-201 is a dihydropyridine-type calcium channel antagonist previously in clinical trials for the treatment of angina pectoris and hypertension.
Adamtsostatin 16 is an anti-angiogenic 17-amino acid peptide containing type I thrombospondin motifs[1].
Sarafotoxin S6c (SRTX-c) is a potent endothelin-B receptor agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels[1].
Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.Target: 5-HT2 RecepterSarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM [1]. Sarpogrelate lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49) [2]. After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate-induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD [3].
2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid is a ketone compound extracted from patent WO2002030860A2, compound example II-9. 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid can be used for the research of cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders[1].
Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant.Target: Serine ProteaseTranilast (FUT-175) is an antiallergic drug for bronchial asthma. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis. It has also been investigated for use as an antiproliferative drug on drug-eluting stents.A 20-40 mg/h dose of FUT-175 prolonged coagulation time sufficiently in the instrumental blood of the extracorporeal circuit but not in the systemic blood. Its anticoagulant activity decreased immediately after hemodialysis. Therefore, we could manage all patients without any bleeding trouble during hemodialysis with FUT-175 as an anticoagulant. Although there were side effects of FUT-175, such as nausea, vomiting, itching and eruption, they were not serious, and FUT-175 could be administered without interruption. FUT-175 seems to be useful as an anticoagulant during hemodialysis for patients susceptible to bleeding.
Pravastatin lactone is a potent HMG-CoA inhibitor. Pravastatin Lactone is a metabolite of pravastatin. Pravastatin lactone reduces blood cholesterol levels by inhibiting cholesterol synthesis[1].
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
GPVI antagonist 3 (Compound 2) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 3 are, respectively, 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin and 51.74 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 3 is a promising antiplatelet agent[1].
FR 58664 is a drug to treat heart failure disease.
Neldazosin is a potent alpha1-adrenoceptor antagonist[1].
Rhamnocitrin is a flavonoid isolated from astragalus complanatus R. Br. (Sha-yuan-zi)[1]. Rhamnocitrin is a scavenger of DPPH with an IC50 of 28.38 mM. Rhamnocitrin has anti-oxidant, anti-inflammatory and an-tiatherosclerosis activity[2].
Scandenolide is a sesquiterpene lactone that can be found in Philippines medicinal plant Mikania cordata. Scandenolide inhibits leukotriene and platelet activating factor synthesis in leukocytes[1][2].
GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects[1].
Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Eptifibatide is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class.Target: OthersEptifibatide is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets [1, 2].
Angiotensin I/II (4-8), a major metabolite of Angiotensin II, is a C-terminal 4-8 pentapeptide[1].
Phosphoramidon, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively[1][2][3].
Trandolapril(RU44570) is an ACE inhibitor used to treat high blood pressure.Target: ACETrandolapril is an ACE inhibitor used to treat high blood pressure, it may also be used to treat other conditions. Trandolapril acts by competitive inhibition of Angiotensin Converting Enzyme (ACE), a key enzyme in the renin-angiotensin system (RAS pathway) which plays an important role in regulating blood pressure. From Wikipedia.
Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.Target: HCN Channel blockerCilobradine is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of Cilobradine. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM Cilobradine (8 ± 2% inhibition; n = 4).