Udenafil(DA8159) is a PDE5 inhibitor used in urology to treat erectile dysfunction.Target: PDE5Udenafil is an oral PDE5 inhibitor. Udenafil significantly increased cAMP and cGMP levels and were more highly distributed in the prostate than plasma. The T/P ratio of udenafil was higher than tadalafil. These findings may help in the assessment of the feasibility of using PDE5 Is to concurrently treat both LUTS and erectile dysfunction [1]. After 12 weeks of treatment, the patients treated with udenafil showed significantly greater change from baseline in the IIEF-EF domain score compared with placebo (placebo, 0.20; 100-mg udenafil, 7.52; and 200-mg udenafil, 9.93, respectively) (P < 0.0001). udenafil significantly enhanced the rates of successful penetration (SEP Q2) and maintenance of erection (SEP Q3) (P < 0.0001) [2].
TLR7 agonist 10 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
Quercetin-3-glucoside is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties.Quercetin-3-glucoside alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway[1].Quercetin-3-glucoside regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Quercetin-3-glucoside has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies[2].
Peonidin-3-O-arabinoside chloride (Compound Ⅻ) is an anthocyanin that can be isolated from Vaccinium myrtillus L.[1].
Oxantel (CP-14445), a m-oxyphenol derivative of Pyrantel (HY-12641), is a N-subtype AChR agonist. Oxantel is an anthelmintic, with excellent trichuricidal properties[1][2].
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1].
rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB1 receptor antagonist. rel-O-2050 also decreases food intake in mice[1].
A small molecule that rapidly downregulates abscisic acid (ABA)-dependent gene expression (IC50=3 and 1.5 uM for RD29B and RAB18 promoters), also inhibits ABA-induced stomatal closure; stimulates expression of plant defense-related genes, major early regulators of pathogen-resistance responses, including EDS1, PAD4, RAR1, and SGT1b, are required for DFPM-interference with ABA signal transduction, disrupts cytosolic Ca(2+) signaling and downstream anion channel activation in a PAD4-dependent manner.
(25R)-Ruscogenin-3-yl α-L-rhamnopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→4)]-β-D-glucopyranoside (compound 1) is a steroidal saponin , can be isolated from the roots of Ophiopogon japonicus[1].
Boc-N-PEG5-C2-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Demethylcantharidate disodium, an endogenous metabolite, induces apoptosis in hepatocellular carcinoma cells via ER stress. Demethylcantharidate disodium shows excellent anticancer activity against multiple types of cancer[1].
Glutarylcarnitine is the diagnostic metabolite for malonic aciduria and glutaric aciduria type I monitored in most tandem mass spectrometry newborn screening programmes.
A small molecule inhibitor of HECT-type ubiquitin ligase with IC50 of 6.8/6.3/6.9 uM for Smurf2/Nedd4/WWP1, respectively; does not block E2 binding but causes a conformational change that results in oxidation of the active site Cys; is active against a range of HECT ligases but does not perturb the ubiquitin system more generally.
H-Thr-Arg-OH is a biologically active peptide.
INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.
A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11[1].
Veratraldehyde is an important chemical used in perfumery, agrochemical, and pharmaceutical industries.
Pyridoxine is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanoma cells. Epirosmanol also exhibits DPPH radical scavenging activity[1][2].
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].
Boc-D-Ala(3,3-diphenyl)-OH is a phenylalanine derivative[1].
4-Methoxybenzimidamide is a reagent used for the determination of reducing carbohydrates and glycoproteins.
N2-iso-Butyroyl-2’-fluoro-2’-deoxyarabinoguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
α-Viniferin is an anti-inflammatory compound from Caragana chamlagu root[1].
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders[1][2].
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3].
MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.
EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259)[1].
Culmerciclib maleate is a cyclin dependent kinase (CDK) inhibitor, and has antineoplastic activity[1].