PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].
Ovalbumin (154-159) is a fragment from ovalbumin. Ovalbumin (154-159) is a potent angiotensin-converting enzyme (ACE) inhibitor. Ovalbumin (154-159) can be used for research of hypertension[1][2].
Resorcinolnaphthalein is a specific angiotensin-converting enzyme 2 (ACE2) enhancer and activates ACE2 activity with an EC50 value of 19.5 μM. Resorcinolnaphthalein can be used for the investigation of hypertension and renal fibrosis[1].
Fenoldopam-d4 (SKF-82526-d4) mesylate is the deuterium labeled Fenoldopam mesylate. Fenoldopam (SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist[1][2].
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca2+ influx through voltage-gated Ca2+ channels, leading to the reduction in [Ca2+]i in vascular smooth muscle cells and consequent peripheral vasodilation[1]. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM[2].
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively[1]. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM)[2].
TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation[1].
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors[1].
TRC051384 hydrochloride is a potent inducer of heat shock protein 70 (HSP70). TRC051384 hydrochloride exhibits protective effects against neuronal trauma via inhibition of necroptosis. TRC051384 hydrochloride can be used for the research of ischemic stroke[1][2].
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver[1]. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension[2].
TRPC3/6-IN-1 is a potent selectivity and orally active molecule blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure[1].
GSK-121 Trifluoroacetates a selective PAD4 inhibitor[1].
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a humanized monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 µg/mL and strongly inhibits cell adhesion[1][2][3].
Piperlotine C is an alkaloid isolated from Piper lolot, with anti-platelet aggregation induced by arachidonic acid, and the IC50 is 26.6 µg/mL[1].
AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.IC50 value: 3.0 ug/kg/min(EC50) [1]Target: P2Y12 receptor inhibitorAZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses that induced a larger than 3-foldincrease in bleeding time were 33 and 100 μg/kg/min for 3 and 13, respectively. Thus, the therapeutic index (TI) was ≥10 forboth compounds. On the basis of these data, compound 3 was progressed into human clinical trials as candidate drug AZD1283.
Aspartic acid calcium (Calcium L-aspartate) is a chelate where calcium is attached to an amino acid naming L-Aspartic acid. L-Aspartic acid is an amino acid and serves as a building block for proteins in the body.
ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) is the 3-24 fragment of adrenocorticotropic hormone (ACTH). ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) can be used for research of a variety of diseases, including cancer, immune diseases, cardiovascular disease[1].
Nepicastat Hcl(SYN117 Hcl; RS-25560-197 Hcl) is a dopamine beta-hydroxylase inhibitor with IC50 of 8.5 ± 0.8 and 9.0 ± 0.8 nM for bovine and human, respectively. IC50 value: 8.5/9.0 nM(bovine/human dopamine beta-hydroxylase)Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine. Nepicastat (SYN117; RS-25560-197) has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such.
Raspberry ketone is a major aromatic compound of red raspberry, widely used as a fragrance in cosmetics and as a flavoring agent in foodstuff; also shows PPAR-α agonistic activity.
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis[1].
3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research[1].
Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696.
Metolazone-d7 is deuterium labeled Metolazone. Metolazone (SR-720-22) is primarily used to treat congestive heart failure and high blood pressure.
Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action.
JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM. JNJ 303 does not have any effects on other cardiac channels at concentrations of 3.3 μM for INa, Ica, Ito, and IKr. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP)[1].
Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.Target: Type-1 angiotensin II receptorCandesartan is generally well tolerated and significantly reduced cardiovascular deaths and hospital admissions for heart failure. Ejection fraction or treatment at baseline did not alter these effects [1]. In rats, TCV-116 inhibited the pressor responses to Ang I, Ang II, and Ang III without an effect on the bradykinin (BK)-induced depressor response. In SHR, the antihypertensive effect of TCV-116 (10 mg/kg) was larger than the maximum antihypertensive effect of enalapril and was not intensified by combination with enalapril. TCV-116 is more effective than enalapril in reducing blood pressure in SHR and 1K, 1C-HR, and that the BK- and/or prostaglandin-potentiating effect of enalapril contributes little to its antihypertensive mechanism in SHR [2].
TC-I 15 (TC-I-15) is an allosteric, collagen-binding integrin α2β1 inhibitor with IC50 values of 26.8 μM and 0.4 μM for GFOGER and GLOGEN, respectively. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition[1].
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β
Apelin-13 is the endogenous ligand of the orphan G protein-coupled receptor APJ, activates APJ receptor with an EC50 value of 0.37 nM in CHO cells[1][2].
Omecamtiv mecarbil is a cardiac myosin activator.