Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
13-Hydroxylupanine Hydroxylupanine is the typical alkaloid profile of sweet lupins. 13-Hydroxylupanine Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle[1].
Lidocaine hydrochloride hydrate (Lignocaine hydrochloride hydrate) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia[1][2].
Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Lercanidipine is a calcium channel blocker of the dihydropyridine class.Target: Calcium ChannelLercanidipine is a calcium channel blocker of the dihydropyridine class, which works by relaxing and opening the blood vessels allowing the blood to circulate more freely around the body. Lercanidipine was effective and well-tolerated in patients with mild-to-moderate hypertension in the daily practice. The effectiveness and safety of the drug were independent of the degree of cardiovascular risk [1, 2].
5-O-Methylembelin is a natural isocoumarin that inhibits PCSK9, low-density lipoprotein receptor (IDOL), and sterol regulatory element binding protein 2 (SREBP2) mRNA expression[1].
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
Guancydine (Guancidine) is an antihypertensive agent[1].
Euphorbetin, isolated from the ethyl acetate extract of the dried whole plants of Viola yedoensis Makino, exhibits anticoagulant activities[1].
Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.
LevCromakalim is an ATP-sensitive K+ channel (KATP) activator.
Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K+ current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent[1].
Gap 26 is a connexin mimetic peptide corresponding to the residues 63-75 of connexin 43, which is a gap junction blocker.
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
GP2-114 (GP-2-114) produces current-dependent cardiovascular action when administered by transdermal iontophoresis.
2-Deacetoxytaxinine B is a potent antiplatelet agent[1].
LpxC-IN-9 (compound 19) is a potent LpxC inhibitor. LpxC-IN-9 has antibacterial and hypotensive effects[1].
3HOI-BA-01 is a mammalian targeting effective rapamycin activation inhibitor.
PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells; shows no general effect on the secreted and intracellular proteome; induces the ribosome to stall around codon 34, mediated by the sequence of the nascent chain within the exit tunnel; reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.
Benazepril-d5 (hydrochloride) is deuterium labeled Benazepril (hydrochloride).
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity[1]. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase[2].
Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, potently inhibits the activity of VEGF-C/D, which are the proangiogenic factors, inhibiting angiogenesis and vascular leakage. Sozinibercept also inhibits diabetic retinal edema in rats[1][2][3].
U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of thromboxane A2 (TXA2) and acts as a potent TXA2 agonist[1].
Zedoarondiol, a sesquiterpene lactone compound, with antioxidant and anti-inflammatory activity. Zedoarondiol can be used for atherosclerosis research[1][2].
MPC1304 is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease[1].
Sapropterin dihydrochloride is a synthetic form of BH4 that is approved for the treatment of BH4 responsive PKU. (1) Sapropterin dihydrochloride can stimulate TH and TPH activities leading to improved dopamine and serotonin synthesis despite persistently elevated brain phenylalanine.(2) Sapropterin dihydrochloride is used to lower blood phenylalanine levels in tetrahydrobiopterin-responsive phenylketonuria in conjunction with a phenylalanine-restricted diet.
3-Epidehydrotumulosic acid has inhibitory activity against AAPH-induced lysis of red blood cells[1].