Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[1][2].
Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1].
Gonadoliberin (GnRH) is a synthetic GnRH. Gonadoliberin binds to GnRH receptor on the cell surface of the gonadotrope, and activates the synthesis and release of LH and FSH[1][2].
Norgestrienone, progestin or synthetic progestin, is a progestin receptor agonist. Norgestrienone is often used as a progestational compound in birth control pills and can be used in combination with ethinyl estradiol[1].
Baxdrostat is a aldosterone synthase inhibitor[1].
Oxytocin (α-Hypophamine) acetate is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research[1].
L-Epinephrine is a hormone secreted by the medulla of the adrenal glands. L-Epinephrine is an α-adrenergic and β-adrenergic receptor agonist.
YCT529 is a potent, selective and orally active RAR-α inhibitor[1].
Impurity of Doxercalciferol is an impurity of doxercalciferol, which is a synthetic analog of ergocalciferol (vitamin D2), used as a drug for secondary hyperparathyroidism and metabolic bone disease, and it suppresses parathyroid synthesis and secretion.
AZD-4818 is a potent antagonist of chemokine CCR1. AZD-4818 can be used for the treatment of chronic obstructive pulmonary disease (COPD) [1].
Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects.
CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1，with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor，particularly androgen receptor，dependent diseases and conditions，such as prostate cancer[1].
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity[1].
LH-RH (7-10) is a tetrapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (7-10) produced in macrophages, type I-like and type II pneumocytes[3].
MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake[1].
LGD-4033 is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.IC50 value: 1 nM (Ki, for androgen receptor) Target: androgen receptorin vitro: LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, binds androgen receptor with high affinity and selectivity.in vivo: LGD-4033 has demonstrated anabolic activity in the muscle, anti-resorptive and anabolic activity in bone, and robust selectivity for muscle versus prostate In animal models. LGD-4033 is well tolerated, has a long elimination half-life and dose-proportional accumulation upon multiple dosing. LGD-4033 is safe, has favorable pharmacokinetic profile, and increases lean body mass even during this short period without change in prostate-specific antigen.
Mepixanox is an analeptic drug used in respiratory and cardiorespiratory insufficiency.
Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
(R)-Avanafil ((R)-TA1790) is a selective PDE5 inhibitor (IC50: 5.2 nM). (R)-Avanafil can be used for research of erectile dysfunction[1].
SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily[1][2].
Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.Target: β-2 Adrenergic ReceptorRitodrine is a tocolytic drug, used to stop premature labor. Ritodrine can significantly prolong a short interval more quickly but with relatively more side effects than magnesium sulphate. Stratified RCTs for different gestational ages and different labour stages should be designed for further study [1]. Ritodrine is a beta-2 adrenergic receptor agonist - a class of medication used for smooth muscle relaxation. Since ritodrine has a bulky N-substituent, it has high β2-selectivity. Also, the 4'-hydroxy on the benzene ring is important for activity as it is needed to form hydrogen bonds. However, the 4'-hydroxy makes it susceptible to metabolism by COMT. Since it is β2-selective it is used for premature labor [2].
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour[1].
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin[1].
Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression[1][2][3].
N-Methylcorydaldine, an alkaloid, shows promising anti-secretory activity[1].
Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer[1][2][3].
2-Phenyl-2-(2-pyridyl)acetonitrile is the major metabolite of SC 15396 metabolized by the supernatant fraction of rat liver homogenate. SC 15396 is an antigastrin that inhibits gastric secretion[1].
Carboprost tromethamine is the synthetic 15-methyl analogue of prostaglandin F2α. Carboprost tromethamine can effectively promote law contraction of the uterus and significantly reduce the amount of bleeding during and after delivery[1][2].