Magnesium oleate is a food additive, anticaking and emulsifying agent. It has also being shown that environmentally friendly multifunctional metal (magnesium) oleate detergent with antioxidation property has good potential for application in synthesizing a variety of substrate detergents.

1,3-Dicyclohexylurea (DCU) is a potent endogenous inhibitor of soluble epoxide hydrolase (sEH), that has been found in human serum. Soluble epoxide hydrolase has been implicated in cardiovascular disease and inflammation in mammals. Endogenously produced 1,3-dicyclohexylurea may have physiological significance via regulation of soluble epoxide hydrolase activity in vivo.

PKI166 is a potent and selective EGFR kinase inhibitor (IC50 = 0.7 nM). PKI166 was tested in phase I clinical trials in patients with advanced solid malignancies, where the recommended dose for further studies was 750 mg once daily for 2 weeks every 4 weeks. In preclinical model, PKI166 was tested in pancreatic, prostate, renal cell, colorectal and other types of cancer. The development of PKI166 was discontinued in 2002 after phase II clinical trials. PKI166 possess antihypertensive properties demonstrated in rat hypertensive chronic kidney disease model.

SDZ-WAG-994 is a potent and selective A1 receptor agonist, discovered by Sandoz. SDZ-WAG-994 was able to induce a dose-related and sustained fall in blood pressure and heart rate in spontaneously hypertensive rats. The compound was investigated in patients with heart failure symptoms and moderate left ventricular systolic dysfunction, where it produced no effect. In patients with patients with permanent atrial fibrillation, SDZ-WAG-994 was able to limit the increase in mean heart rate during exercise. The compound was also tested for treatment of postoperative dental pain, but for all efficacy measures, SDZ-WAG-994 was not significantly different from placebo.

E-3174 is an active carboxylic acid metabolite of losartan and is an antagonist of the angiotensin II receptor, type 1 (AT1). Losartan was the first orally active AT1 receptor antagonist available on the market, and it is the antagonist with which the greatest clinical experience has been accumulated. EXP3174 is 10 to 20 times more potent than losartan and has a longer duration of action than losartan. However, the oral bioavailability of EXP 3174 is very low. Thus, the drug on the market is losartan, but most of the losartan’s antihypertensive effect is due to EXP 3174.

Germine is an alkaloid that occurs in Veratrum and Zygandenus species. The drug, like veratrine and veratridine, induces repetitive discharges in nerve cells, seemingly because of derangements in sodium channel function. Germine may be used medically as an antihypertensive agent. Germine has being shown to have antitumor activity against Hh-dependent lung cancer cell lines, SW1990 and NCI-H249.

Cinnamyl alcohol (CAL, 3-phenyl-2-propen-1-ol) is found mostly in esterized form as a natural component in cinnamon oil obtained from the bark of the Cylonese cinnamon tree. Furthermore, (esterized) CAL is a component of the balsam of Peru from Myroxylon pereirae, of Styrax (balsam) from the wood of Liquidambar orientalis Miller or Liquidambar styraciflua L. and further plant extracts. The regulatory status of CAL includes approval (21 CFR 172.515) by the FDA and Generally Recognized as Safe (GRAS) as flavor ingredient [Number 2294] by the Flavor and Extract Manufacturers
Association. CAL included in the Council of Europe
s list of substances which may be used in foodstuffs. CAL have been reported as common component of food occurring mainly in a wide variety of fruits, vegetables, and spices in varying concentrations. The plant phenolic CAL is used as a fragrance ingredient and has antipyretic and antiproliferative effects. A recent report also demonstrated its vasodilatory activity.

Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It acts on the renin-angiotensin system in two ways to decrease total peripheral resistance. First, it blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle, causing vascular dilatation. Second, it inhibits sympathetic norepinephrine production, further reducing blood pressure. Eprosartan is indicated for the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).

Mibefradil is a calcium channel blocker, chemically unlike other compounds in the class, that was approved by the Food and Drug Administration (FDA), U.S.A. in June 1997 for the treatment of patients with hypertension and chronic stable angina. Shortly following its introduction, mibefradil was withdrawn from the market in the U.S.A. as well as in Europe. The reason for the voluntary withdrawal of the drug by Roche laboratories was claimed to be the result of new information about potentially harmful interactions with other drugs. Mibefradil is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 uM and 18.6 uM for T-type and L-type channels respectively. Mibefradil is a tetralol calcium channel blocking agent that inhibits the influx of calcium ions across both the T (low-voltage) and L (high-voltage) calcium channels of cardiac and vascular smooth muscle, with a greater selectivity for T channels. Vasodilation occurs in vascular smooth muscle, causing a decrease in peripheral vascular resistance and a resulting decrease in blood pressure. Mibefradil causes a slight increase in cardiac output during chronic dosing. Mibefradil slows sinus and atrioventricular (AV) node conduction, producing a slight reduction in heart rate and a slight increase in the PR interval. It has also been shown to slightly lengthen the corrected sinus node recovery time and AH interval and to raise the Wenckebach point. The mechanism by which mibefradil reduces angina is not known, but is thought to be attributed to a reduction in heart rate, total peripheral resistance (afterload), and the heart rate-systolic blood pressure product at any given level of exercise. The result of these effects is a decrease in cardiac workload and myocardial oxygen demand. Mibefradil has been repurposed from an abandoned antihypertensive to a targeted solid tumor treatment, and it has been rescued from drug-drug interactions by using short-term dose exposure. Tau is using the early success of mibefradil as a proof of concept to build a platform technology of Cav3 blockers for broad antitumor applications in combination with new targeted cancer therapies, well-established.

Spirapril (Renormax) is an ACE inhibitor antihypertensive drug used to treat hypertension. Spiraprilat, the active metabolite of spirapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Spiraprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.