A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells[1].
APJ receptor agonist 4 is a potent and oral active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease[1].
Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2 (Ang2) with high affinity, but shows no binding to Ang1[1].
N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor[1][2].
MAHMA NONOate is a NO donor. MAHMA NONOate effectively inhibits platelet aggregation induced by either collagen or ADP[1].
5-Amino-4-oxopentanoic acid is a non-protein amino acid that plays a rate-limiting role in heme biosynthesis.
Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables; has shown anticancer and cardioprotective activities.
SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
[Sar1, Ile8]-Angiotensin II is a peptide that has multiple effects on vascular smooth muscle, including contraction of normal arteries and hypertrophy or hyperplasia of cultured cells or diseased vessels.
Asobamast is a potent, orally active antiallergic agent that inhibits ige mediated passive pulmonary allergic responses in rats (ED50=4.7 mg/kg) and inhibits antigen-induced mediator release from sensitized guinea pig lung fragments[1].
ML359 is a small molecule, specific inhibitor of Protein disulfide isomerase (PDI) with IC50 of 250 nM; displays >100-fold selectivity over other thiol isomerases (Erp5, Thioredoxin, Thioredoxin reductase); shows no cytotoxicity in three human cell lines, and some activity in inhibiting platelet aggregation in vitro.
Ranibizumab (RG-6321) (anti-VEGF) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165)[1]. Ranibizumab (anti-VEGF) slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research[1].
Glycerol-2-13C is the 13C labeled Glycerol. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis[1][2][3][4].
A-58365B is an Angiotensin-converting Enzyme (ACE) inhibitor. A-58365B has antihypertensive effects[1].
CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor, which inhibits CETP-mediated transfer of cholesteryl ester in human serum with an IC50 of 2.3 nM[1].
Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity[1][2].
18-Deoxyherboxidiene (RQN-18690A) is a potent angiogenesis inhibitor. 18-Deoxyherboxidiene targets SF3b, a spliceosome component that is a subcomplex of the U2 small nuclear ribonucleoprotein (snRNP) in the spliceosome. 18-Deoxyherboxidiene inhibits the migration and tube formation of human umbilical vein endothelial cells (HUVECs) without significant cell toxicity. 18-Deoxyherboxidiene has the potential for cancer research[1].
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively.
Lemildipine is a new dihydropyridine calcium entry blocker.
Isosorbide mononitrate(Isosorbide-5-mononitrate) is a nitrate-class compound used for angina pectoris; acts by dilating the blood vessels so as to reduce the blood pressure.
1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a quinolone alkaloid, is a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, with IC50s of 20.1 μM and 34.1 μM, respectively. 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone shows potent anti-Helicobacter pylori activity with the MIC of 10 μg/mL[1][2][3].
Mexiletine hydrochloride is a non-selective voltage-gated sodium channel blocker; Class IB anti-arrhythmic compound.
ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 µM and 1.7 µM respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy[1][5].
Acremonidin A is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremonidin A binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 19.40 nM[1].
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3].
Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
Vardenafil Hcl is a PDE5 inhibitor used for treating erectile dysfunction.Target: PDE5Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM. Relative to PDE5, the ratios of the IC50 for PDE1 were 257 (60), for PDE6 16 (7.4). Vardenafil significantly enhanced the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle [1]. Both vardenafil doses(10 mg or 20 mg) significantly enhanced the
N-Methyldopamine hydrochloride is a precursor of adrenaline in the adrenal medulla. N-Methyldopamine hydrochloride is a modification of the dopamine (DA), and retains agonist activity at the DA1 receptor. N-Methyldopamine hydrochloride remains capable of universal surface coating and secondary reactions using the surface catechols. N-Methyldopamine hydrochloride can be used for heart failure research[1][2][3].
Terlipressin is a potent vasoconstrictor that acts via V1 receptors on arteriolar smooth muscle cells. Terlipressin can result in splanchnic vasoconstriction augmenting systemic arterial blood pressure with beneficial circulatory and renal effects that would be expected to also ameliorate the key pathophysiological changes responsible for the development of refractory ascites
TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system[1].