ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is ＞25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively[1].
Xanthine oxidase is a xanthine oxidoreductase enzyme that generates reactive oxygen species (ROS), catalyzes the oxidation of hypoxanthine to xanthine, and further catalyzes the oxidation of xanthine to uric acid[1].
Testosterone tridecanoate is a prodrug of testosterone. Testosterone is the primary male sex hormone and an anabolic steroid.
Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
(+)-Phenserine is a novel selective cholinesterase noncompetitive inhibitor with an IC50 of 45.3 μM.
Norfenefrine is an orally active, endogenously found α-adrenergic agonist and can be used for the research of female stress incontinence[1][2].
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controlling acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock treatment[1][2][3][4][5].
Norethynodrel (Enidre) is a 19-nortestosterone derivative to be used as a progestagen. Norethynodrel can be used for researching inhibition of ovulation[1].
Tabimorelin (NN703) hemifumarate is an orally active growth hormone (GH) secretagogue. Tabimorelin hemifumarate is also a potent inhibitor of CYP3A4 activity[1].
Peroxidase actively involves in oxidizing reactive oxygen species, innate immunity, hormone biosynthesis and pathogenesis of several diseases[1].
17α-Hydroxyprogesterone acetate possesses progestational activity. 17α-Hydroxyprogesterone acetate has antiinflammatory effects at the murine maternal-fetal interface[1][2].
EP2 receptor antagonist-2 (CID891729) is an antagonist of EP2 receptor. EP2 receptor antagonist-2 inhibits the EP2 receptor activation induced by PGE2. EP2 receptor antagonist-2 also suppresses lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA)[1].
Androstenediol 17-acetate is a synthetic anabolic-androgenic steroid and an androgen ester.
Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3].
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
Thioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study[1][2].
Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].
Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation[1][2].
Treprostinil palmitil (TP) is the prodrug of DP1 and EP2 agonist, Treprostinil (UT-15), whose EC50 values were 0.6 and 6.2 nM, respectively. Treprostinil palmitil is a pure prodrug and possesses no inherent binding to G-protein coupled receptors including prostanoid receptors[1][2].
Sodium tauroglycocholate is an inhibitor of the biliary acid transporting system of the hepatocyte and also a surfactant used as a chemical permeation enhancer.
SLU-PP-1072 is a dual ERRα/γ inverse agonist, used in Prostate cancer (PCa) research. SLU-PP-1072 disrupts PCa cell metabolism, and induces apoptosis via dysregulating cell cycle[1].
Lacto-N-biose I (Galβ1-3GlcNAc), as an endogenous metabolite, is an acceptor for the α1,2-fucosyltransferase enzyme from Helicobacter pylori[1].
13-hydroxyoctadecadienoic acid (13-HODE) is an endogenous lipoxygenase metabolite of Linoleic acid (HY-N0729). 13-hydroxyoctadecadienoic acid stimulates prostacyclin production by enhancing arachidonic acid (AA) release from phospholipids[1].
Substituted piperidines-1 is a compound that can promote the release of growth hormone in humans and animals.
Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity[1][2][5].
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain[1].
a-Helical Corticotropin Releasing Factor (12-41) is a 30 amino acids long, α-helical analogue of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, which stimulates the secretion of adrenocorticotrophic hormone (ACTH). a-Helical Corticotropin Releasing Factor (12-41) would suppress the stimulatory effect[1][2].
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Sotalol D6 hydrochloride is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is a non-selective competitive β-adrenergic receptor antagonist that also exhibits Class III antiarrhythmic properties by its inhibition of potassium channels[1][2].