NHS-PEG1-SS-PEG1-NHS is a reversible linker for biomacromolecule link with active small molecule. NHS-PEG1-SS-PEG1-NHS can be used in proteins liposomes or nanoparticles[1].
LPLRF-NH2 is a member of RFamide peptide with anorexigenic effect. LPLRF-NH2 increases arterial blood pressure and modulates the electrical activity of brainstem neurons[1][2][3].
Cinepazide is a vasodilator.Target: OthersCinepazide is a vasodilator. Cinepazide (30 mg/kg, i.v.) potentiated the vertebral vasodilator response of dogs to intravertebral adenosine and cyclic AMP, Intravertebral cinepazide(1-10 mg) increased vertebral blood flow in a dose-related manner and the effect was partially inhibited by intravenous pretreatment with aminophylline but not by pretreatment with autonomic antagonists. Cinepazide resembled cinnarizine and papaverine in that the drug antagonized rabbit aortic contraction induced by KCl, norepinephrine or CaCl2 [1]. Cinepazide in concentrations ranging from 10-6 to 10-5M augmented the relaxing responses to ATP, adenosine and cAMP. However, this agent did not affect the relaxations induced by isoproterenol and papaverine and the contractions induced by 5-HT, prostaglandin F2α and ATP. cinepazide selectively potentiates the relaxing response mediated through purinergic P1 receptors [2].
ONO-4817 is a potent inhibitor of matrix metalloproteinase (MMP). Inhibition of matrix metalloproteinases (MMPs) is expected to suppress atherosclerotic neointimal proliferation and thus limits atheromatous plaque progression. ONO-4817 suppresses the development of aortic intimal hyperplasia in experimental hyperlipidemic rabbit[1].
Macitentan D4 (ACT-064992 D4) is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan is used for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis[1].
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier[1][2].
L-Isoleucyl-L-arginine is a dipeptide formed from L-isoleucine and L-arginine residues. L-Isoleucyl-L-arginine is a potent angiotensin-converting enzyme (ACE) inhibitor. L-Isoleucyl-L-arginine can be used for research of hypertension[1].
HS56 (Pim-DAPK3 inhibitor HS56) is a potent, dual Pim/DAPK3 inhibitor with Ki of 72 nM (Pim-3) and 315 nM (DAPK3), shows micromolar potency toward Pim-1 and Pim-2 (Ki=1.5 and 17 uM); displays a high degree of selectivity for DAPKs and Pims against a panel of 468 kinases, with only two off-target interactions TYK2 and GAK; also displays no significant inhibition or activation of nicotinic, adrenergic, or muscarinic receptors at 10 uM; HS56 delayed force onset, decreased contractile force, and reduced LC20 phosphorylation in excised rat caudal arterial VSM tissues, lowers blood pressure in spontaneously hypertensive mice without affecting heart rate.
Naminidil is a cyanoguanidine KATP opener.
Anipamil is a long-acting calcium channel blocker, used for the treatment of cardiovascular disease.
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM[1]. Antianemia agent[1].
Plasma kallikrein-IN-3 is a plasma kallikrein inhibitor (IC50: 0.15 μM). Plasma kallikrein-IN-3 can be used for hereditary angioedema, diabetic macular edema, and diabetic retinopathy research[1].
Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.
Hexacosanoic acid-d4-1 is the deuterium labeled Hexacosanoic acid. Hexacosanoic acid is a long-chain fatty acid related to various diseases such as adrenoleukodystrophy (ALD), adrenomyeloneuropathy (AMN) and atherosclerosis.
Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
Fluvastatin (Leschol) inhibits HMG-CoA reductase activity with IC50 of 8 nM.IC50 value: 8 nMTarget: HMG-CoA reductaseFluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Human hepatocellular carcinoma cell (HCC) studies indicate that Fluvastatin induces G2/M phase arrest. In the presence of Fluvastatin, HCC cells show a decrease of Bcl-2 and procaspase-9 expression, and an increase in Bax, cleaved caspase-3, and cytochrome c. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
Guanabenz is an orally active α-2-adrenoceptor agonist, has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure[1].
Pinacidil is a potent activator of potassium channel. Pinacidil is an antihypertensive agent which hyperpolarises vascular smooth muscle by opening K+-channels. Pinacidil significantly improves the reperfusion function and cardiac compliance. Pinacidil has direct cardioprotective efficacy[1].
Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator[1].
Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
Acetyl-coenzyme A (Acetyl-CoA) lithium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A lithium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A lithium is also a key precursor of lipid synthesis[1][2][3][4].
KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
Diltiazem is an orally active L-type Ca2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].
Eltrombopag is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.
TA-7552 is a potent cholesterol-lowering agent.
TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).
Bepridil hydrochloride (CERM 1978) is a calcium channel blocker, with antianginal activity.
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2].