SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model[1][2][3][4][5].
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether has been proposed as a mild warming agent providing a warming sensation and enhancing the blood circulation[1].
RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values are 8.7 and 8.9 respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.IC50 value: 8.7(pKi, 5-HT1E); 8.9 (pKi, 5-HT1F) Target: 5-HT1E/1F receptorin vitro: BRL 54443 is a potent 5-ht1E/1F receptor agonist (pEC50 values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pKi values are 8.7. 8.9, 7.2, 6.9, 7.2, 5.9, 7.0, 6.5, < 6, < 6, 6.3 and 6.2 for human 5-HT1E, 1F, 1A, 1B, 1D, 2A, 2B, 2C, 4, 7, D2 and D3 receptors respectively). Induces 5-HT2A receptor-mediated mouse aortic contraction in vitro (pEC50 = 6.52). Active in vivo. In DG membranes, BRL54443, a 5-ht(1E) /5-HT(1F) agonist, selectively stimulated 5-ht(1E) receptors and potently inhibited forskolin-dependent cAMP production (IC50 = 14 nM) [2]. The 5-HT(1E/1F) receptor agonist BRL 54443 also induced contraction (-log EC(50) = 6.52) [1].in vivo: Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats [3].
Urotensin II (114-124), human, an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
Cilazapril Monohydrate is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.Target: ACECilazapril is a new nonthiol group containing angiotensin converting enzyme (ACE) inhibitor. Cilazapril has been investigated in more than 4000 patients with all degrees of hypertension, as well as in the special patient groups such as the elderly, renally impaired, and patients with concomitant diseases, such as congestive cardiac failure or chronic obstructive pulmonary disease [1]. Cilazapril is a very potent and highly effective converting enzyme inhibitor. Doses well below 5 mg/day will probably suffice for therapeutic efficacy [2].
ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
Anagrelide, an inhibitor of phosphodiesterase type III (PDEIII) (IC50=36 nM), inhibits platelet production. Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide plays in the antithrombopoietic action. The platelet-lowering agent[1].
3-(3-Hydroxyphenyl)propionic acid is a flavonoid metabolite formed by human microflora. 3-(3-Hydroxyphenyl)propionic acid shows vasodilatory activity[1].
Hexadecanoate-13C16 potassium is the 13C-labeled Hexadecanoate sodium. Hexadecanoate-13C16 potassium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Amlodipine besylate is a long-acting calcium channel blocker.Target: Calcium ChannelAmlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells. Experimental data suggest amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects, or decreased heart muscle contractility, can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa = 8.6), and its interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. From Wikipedia.
Secoxyloganin, isolated from Lonicera japonica Thunb, inhibits the blood flow (BF) decrease. Secoxyloganin has allergy-preventive activity[1].
Prepro-ANF (56-92), human is a human atrial natriuretic factor precursor. Prepro-ANF (56-92), human is also a Guanylate Cyclase activator that enhances particulate Guanylate Cyclase activity in the renal membrane and renal unit[1].
2'-Ethyl Simvastatin (compound 6) is a Mevinolin analog, with HMG-CoA reductase inhibition[1].
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases[1].
Oxyfedrine hydrochloride, a vasodilator, is an orally active β-adrenoreceptor agonist. Oxyfedrine decreases the tonicity of coronary vessels. Oxyfedrine hydrochloride can be used in the research of cardiovascular disease[1][2].
Gliclazide D4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic[1].
GPRP (Pefa 6003) is a fibrin polymerization inhibitor that inhibits the interaction of fibrinogen with the platelet membrane glycoprotein IIb/IIIa complex (GPIIb/IIIa)[1][2].
Xipamide is a sulfonamide-based diuretic. Xipamide is an antihypertensive agent able to selectively inhibit the anion exchanger (AE)[1].
Nifedipine is a potent calcium channel blocker and drug of choice for cardiac insufficiencies.
Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
Dihydrocurcumenone is a carabrane-type sesquiterpene. Dihydrocurcumenone can be isolated from Curcuma zedoaria, and the common form is 4-dihydrocurcumenone. Curcuma zedoaria sesquiterpene has vascular relaxation activity. 4-dihydrocurcumenone can inhibit the high concentration of K+ induced constriction of isolated rat aortic strips[1].
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
4,6-Dioxoheptanoic acid is a potent inhibitor of heme biosynthesis.
Digitoxin is an effective Na+/K+-ATPase inhibitor, the EC50 value of Digitoxin is 0.78 μM.IC50 value: 0.78 μM (EC50)Target: Na+/K+-ATPasein vitro: Digitoxin shows a significantly cytotoxic effect in H1975 cells by causing G2 phase arrest, also remarkably activates 5' adenosine monophosphate-activated protein kinase (AMPK). Moreover, Digitoxin suppresses microtubule formation through decreasing α-tubulin. Digitoxin effectively depresses the growth of TKI-resistance NSCLC H1975 cells by inhibiting microtubule polymerization and inducing cell cycle arrest. Digitoxin has the highest cytotoxicity in H1975 cells, whose CC50 value was 0.19 ± 0.06 μM. Digitoxin-induced inhibition mechanism is likely due to causing G2/M cell cycle arrest in H1975 cells in dose dependent manners.
Chlophenadione is a potent anticoagulant compound.
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively[1].