R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor. The fuction is similar to R 80122 (HY-100615, Revizinone).In vivo: The administration of Revizinone improved the haemodynamic profile with an increase in cardiac output, a decrease in systemic vascular resistance and a stable heart rate and mean arterial blood pressure. [1] With regard to reconstitution of contractility and cardiac function Revizinone (E-isomer) is 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer). [2] Revizinone significantly increases global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [3]
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity[1].
Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE[1][2].
Lys-Ala-pNA is hydrolytic substrate the of dipeptidyl peptidase (DPP) II with Km of 0.42 mM[1].
Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor[1].
Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator[1][2].
Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively[1].
Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions[1][2].
Nitrefazole is a 4-nitroimidazole derivative with strong and long lasting inhibition of aldehyde dehydrogenase (ALDH), an enzyme involved in the metabolism of alcohol.
MMP-9-IN-3 is a MMP-9 inhibitor (IC50: 5.56 nM) that forms hydrogen bond with MMP-9. MMP-9-IN-3 also inhibits AKT activity (IC50: 2.11 nM). MMP-9-IN-3 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-3 can be used in the research of cancers[1].
ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion[1].
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsin K activity[1][2].
FITC-GW3965 is a fluorescence-labelled liver X receptor β (LXRβ) agonist GW3965 (HY-10627). FITC-GW3965 is a tracer, that can be designed by replacing the trifluoromethyl of GW3965 with an amide to link the FITC. FITC-GW3965 can be used to study the function of LXRβ[1].
Aristololactam IIIa exhibits significant inhibitory effects on superoxide anion generation and elastase release with IC50 values of 0.12 and 0.20 μg/mL, respectively[1].
Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].
SB-3CT is a potent and competitive inhibitor of matrix metalloproteinase (MMP-2) and MMP-9.
An oral glucocorticoid agonist for the treatment of rheumatoid arthritis. Rheumatoid Arthritis Phase 1 Clinical
Imsamotide (IDO194-214) is a Indoleamine 2,3-Dioxygenase (IDO) peptide with sequences of DTLLKALLEIASCLEKALQVF, the IDO194-214. Imsamotide is also an immunological agent for active immunization, as well as an antineoplastic agent[1][2].
FTase-IN-1 (compound 17a) is a potent and specific inhibitor of fanesyl transferase (FTase) with an IC50 of 0.35 μM. FTase-IN-1 displays cytotoxicity potential and antitumor activity[1].
Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
Galegenimab (FHTR 2163; RG 6147; RO 7171009), an anti-High-temperature requirement A1 (HTRA1) antibody fragment. Galegenimab can be used for age-related macular degeneration (AMD) research[1].
Trandolapril (RU44570) hydrochloride is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolapril hydrochlorideat. Trandolapril hydrochloride is an orally active angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI)[1].
Deltasonamide 2 TFA is a PDEδ inhibitor with a Kd of ~385 pM and an EC50 of 1.24 μM[1].
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity[1][2].
Palmitic acid-1,2,3,4-13C4 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid 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].
7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with an IC50 of ~1-3 μM[1].