Prostaglandin B1 (PGB1) is a metabolite of Prostaglandin E1 (HY-B0131). Prostaglandin E1 is a prostanoid receptor ligand[1][2].
Androgen receptor antagonist 9 (compound 28) is an antagonist of the androgen receptor[1].
PTI-428 is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier[1].
Misoprostol(SC29333) is a synthetic prostaglandin E1 (PGE1) analog that is used to prevent gastric ulcers, to treat missed miscarriage, to induce labor, and to induce abortion.Target: Prostaglandin ReceptorMisoprostol is a synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties. Misoprostol seems to inhibit gastric acid secretion by a direct action on the parietal cells through binding to the prostaglandin receptor. Administration of misoprostol to EP3+/+ and EP3-/- mice showed similar levels of infarct rescue, indicating that misoprostol protection was not mediated through the EP3 receptor. Taken together, these findings suggest a novel function for misoprostol as a protective agent in cerebral ischemia acting via the PGE(2) EP2 and/or EP4 receptors [1, 2].
β-Amyrin palmitate shows HMG-CoA reductase inhibition[1]. And β-Amyrin palmitate has anti-diabetes mellitus activity[2].
L-Lysine-13C6,d9,15N2 dihydrochloride is the deuterium, 13C-, and 15-labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
Acetyl Gastric Inhibitory Peptide (human) is a fatty acid derivatized analog of glucose-dependent insulinotropic polypeptide with improved antihyperglycaemic and insulinotropic properties. Acetyl Gastric Inhibitory Peptide (human) can be used for research of diabetes, insulin resistance and obesity[1][2][3].
Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.Target: Estrogen ReceptorEthinyl estradiol (EE), also sometimes written as ethinylestradiol, ethynyl estradiol, or ethinyl estradiol, is a derivative of 17β-estradiol (E2), the major endogenous estrogen in humans. EE is an orally bioactive estrogen used in many formulations of combined oral contraceptive pills. It is one of the most commonly used medications for this purpose. Transdermal ethinyl estradiol carries a greater risk of clot formation and venous thromboembolism than 17 beta estradiol, which some have theorized to be related to different amounts of hepatic metabolism after absorption. The same contraindications and precautions apply for EE as with other estrogen medications.Estinyl was a preparation of EE alone that was used for the management of menopausal symptoms and female hypogonadism. EE is released into the environment as a xenoestrogen from the urine and feces of people who take it as a medication. The major concern with unopposed estrogen is of endometrial cancer. As such, the medication is generally prescribed with progesterone in the setting of birth control. The first orally active semisynthetic steroidal estrogen, EE (17α-ethynylestradiol), the 17α-ethynyl analog of E2, was synthesized in 1938 by Hans Herloff Inhoffen and Walter Hohlweg at Schering AG in Berlin.
Eprotirome is a liver-selective thyroid hormone receptor agonist.
Silodosin-d4 (KAD 3213-d4) is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
L-Lysine-13C6,15N2 hydrochloride is the 13C- and 15N-labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
Norcholic acid is a normal minorbile C23 bile acid having four side chain and exsits in human urine and meconium. Norcholic acid can become prominent under certain pathological conditions. Norcholic acid is efficiently absorbed from intestine and quickly excreted into the bile but not into urine[1].
Exendin-4 (3-39) is a peptide. Exendin-4 (3-39) is a truncated form of Exendin-4 (HY-13443) that lacks the first two amino acids. Exendin-4 is a potent Glucagon-like peptide-1 receptor (GLP-1r) agonist. Exendin-4 (3-39) and Exendin-4 can be used for the research of diabetic and hypothalamic-pituitary-adrenal (HPA) axis[1][2].
Tiratricol is a thyroid hormone analog with hepatic, has been used to suppress pituitary TSH secretion, with attenuation of extrapituitary thyromimetic effects.
NK3R-IN-1 (compound 16x), a imidazolepiperazine derivative, is an orally active Neurokinin Receptor NK3R inhibitor. NK3R-IN-1 decreases blood luteinizing hormone levels in ovariectomy (OVX) model[1].
Granuliberin R is a new mast cell degranulating peptide comes from amphibian, can be isolated from the skin of frog Rana rugosa. Granuliberin R is a dodecapeptide, can act on rat peritoneal mast cell to liberate granules and release histamine[1][2].
(rac)-AG-205 is a potent inhibitor of progesterone receptor membrane component 1 (Pgrmc1) that induces genes involved in sterol synthesis, including the INSIG1 protein, which forms a complex with PGRMC1. (rac)-AG-205 prevents neuronal resistance to hypoxic ischaemia by blocking NF-kB signalling and activation of the BDNF/PI3K/AKT pathway[1].
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) agonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character[1].
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (salmon) is a GnRH analog that induces ovulation and/or spawning in farmed fish[1].
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes[1][2].
Cimbuterol is a β-adrenergic receptor agonist[1].
PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin[1][2].
Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).
Estradiol cypionate is a 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptorIC50 value:Target: estrogen receptorEstradiol cypionate is a synthetic ester, is a estrogen. Compared to other commonly used estradiol esters, via the intramuscular route, Estradiol cypionate is found to have the longest duration of action with a duration of ~11 days,
Bepotastine is an orally active second-generation histamine H1 receptor antagonist. Bepotastine has the potential for allergic rhinitis and urticaria/pruritus treatment[1][2].
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model[1].
Ceramides Mixture is an endogenous ceramide and consists of hydroxy and non-hydroxy fatty acid-containing ceramides. Ceramides Mixture is a main lipid component of the permeability barrier in epidermis. Ceramides Mixture is involved in the regulation of growth inhibition, cell cycle arrest, and modulation of telomerase activity[1][2].
Acyline , a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels[1].
Nestoron(ST1435; Elcometrine) is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor. IC50 value:Tareget: progesterone receptorNestorone acts primarily as a high-affinity agonist of the progesterone receptor. It lacks significant affinity for the androgen receptor, and accordingly, does not produce any androgenic or anabolic effects. It does not bind to the estrogen receptor either. Nestorone does however have some affinity for the glucocorticoid receptor, where it appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. Nestorone does not bind to sex hormone-binding globulin, and is instead bound to serum albumin.