Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
Polythiazide (NSC-108161, P-2525) is used to treat fluid retention (edema) caused by a variety of causes, including congestive heart failure, severe liver disease (cirrhosis), kidney disease, or steroid or hormonal medication.
3-Iodothyronamine is derived from the deiodination and decarboxylation of endogenous thyroxine. It activates the G protein-coupled receptor known as trace amine-associated receptor 1 at nanomolar concentrations whereupon it rapidly influences thyroid hormone actions including body temperature, heart rate, and cardiac output. It has also been reported to function in controlling lipid and glucose utilization, hormonal secretion, and neuronal function, and has been considered for use in chemically-induced hibernation for medical purposes.
Cabergoline diphosphate is a dopamine D2 receptor agonist used for prolactinoma treatment. Cabergoline permits rapid and effective hormonal and tumor control by normalizing prolactin-producing pituitary adenomas levels.
Calcitriol Impurities D (24-Homo Calcitriol) 是维生素的一种激素形式,可促进HL-60人早幼粒细胞白血病细胞分化为单核细胞。Calcitriol Impurities D 具有骨吸收活性,抑制人类免疫缺陷病毒在人体细胞中的复制。Calcitriol Impurities D 具有抗病毒活性们可以用于治疗艾滋病和病毒感染。
Nomegestrol is a progestin. It is used in the treatment of gynecological disorders, in menopausal hormone therapy for the treatment of menopausal symptoms, and in hormonal contraceptives.
Chronic intracerebroventricular (ICV) injection of a VGF peptide named TLQP-21 increased resting energy expenditure and temperature in mice. Furthermore, in mice fed a high-fat diet, the same peptide prevented the increase in body and white adipose tissue
GW5638 is a estrogen receptor ligand. GW5638 is a prodrug of its active metabolite GW7604. GW5638 appears to act as an antagonist in these in vitro systems, although in a manner distinct from other known ER modulators. GW5638 is also classified as a pseud
Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.
Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce afimoxifene (4-hydroxytamoxifen) and endoxifen.
Ascr#7, an ascaroside-based hormonal compound, plays a significant role in nematode physiology. It is specifically expressed throughout the various stages of nematode development. Notably, ascarosides exhibit the capability to initiate the formation of dauer larvae, which are characterized by their long lifespan and exceptional stress resistance.