11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells[1][2].
Triamcinolone Acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone. Target: Glucocorticoid ReceptorTriamcinolone acetonide is a synthetic corticosteroid used to treat various skin conditions, to relieve the discomfort of mouth sores, and in nasal spray form, to treat allergic rhinitis. It is a more potent derivative of triamcinolone, and is about 8 times as potent as prednisone [1].
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively[1].
[Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. [Hyp3]-Bradykinin interacts with B2-bradykinin receptors and stimulates inositol phosphate production in cultured human fibroblasts[1].
Peptide YY (pig) is a 36 amino acid gastrointestinal peptide, can be isolated from porcine duodenum. Peptide YY (pig) decreases appetite and food-intake by activation of the Y2 receptor. Peptide YY (pig) is present mainly in pancreatic endocrine cells with effect on both intestinal motility and the cardiovascular system[1][2][3].
Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent[1][2][3][4].
SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1].
[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Glp1,D-Phe2,D-Trp3,6]-LH-RH acts as a GnRH receptor antagonist[1].
Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
Ludaterone is an antiandrogen agent, with potent antiandrogenic activity[1].
SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor[1].
Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system[1].
Oxytocin antiparallel dimer is the disulfide-bridged homo peptide dimer[1].
Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
Mestranol is the 3-methyl ether of ethinylestradiol. It was the estrogen used in many of the first oral contraceptives.Target: Estrogen Receptor/ERRMestranol is absorbed very rapidly from the digestive tract and maximum plasma levels are attained in 1-4 hours, the majority at 1-2 hours. Detectable levels of mestranol are present 24 hours postingestion in 58% of subjects after a 50 μg dose and in 79% after a 100 μg dose. At all dose levels, highest plasma mestranol levels and area under the curve of plasma levels (AUC) occurred in Sri Lankan women, and lowest plasma levels in Nigerian women, even when corrected for body surface differences [1].
Clomifene hydrochloride is an orally active compound used for infertility. Clomifene hydrochloride is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
L-366682, a cyclic hexapeptide, possesses antagonism of oxytocin[1].
Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives.Target: Progesterone ReceptorA synthetic progestational hormone with actions similar to those of progesterone and about twice as potent as its racemic or (+-)-isomer (norgestrel). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. It is usually supplied in a racemic mixture (Norgestrel, 6533-00-2). Only the levonorgestrel isomer is active. Levonorgestrel is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Triphasil, and Min-Ovral [1].
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease[1].
GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM[1].
Thyrotropin (TSH) is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid[1][2].
Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action[1][2][3].
GHRF, porcine is a growth hormone releasing factor (GHRF) peptide (porcine). GHRF binds to GHSR and induces the release of growth hormone[1][2].
LH-RH II (chicken) is one of the two forms of luteinizing hormone-releasing hormone (LHRH) the hypothalamus of the domestic hen, which are structural variants of mammalian LHRH. LH-RH II (chicken) enhances gonadotrophin release in the domestic chicken[1][2].
Dicentrine is a natural product isolated from the plant Lindera megaphylla with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates[1].
Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has Kis of 100-500 nM for human α2δ-1 subunit of Cav2.2 calcium channel and NET, respectively[1].
Lafutidine-d10 is deuterium labeled Lafutidine. Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease[1].
DL 071IT is a potent non-selective beta-adrenergic receptor blocker. DL 071IT exhibits intrinsic sympathomimetic activity and weak membrane stabilizing activity. DL 071IT reduces exercise heart rate and systolic blood pressure, and even significantly lowers resting heart rate[1].
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].
15-Keto latanoprost is a metabolite of Latanoprost, which is an ocular hypotensive agent[1].