Endocrinology

Cortisone (Standard) is the analytical standard of Cortisone. This product is intended for research and analytical applications. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.

2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.

3,5-Dinitrocatechol (OR-486) is an orally active, blood-brain barrier-permeable selective catechol-O-methyltransferase (COMT) inhibitor. 3,5-Dinitrocatechol can be used in research related to Parkinson's disease, pheochromocytoma and adult cataract.

Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC₅₀ values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.

γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na⁺) balance and blood pressure through activation of the melanocortin receptor 3 (MC3-R).

Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.

Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC₅₀ of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC₅₀ = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE_₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.

Octopamine (hydrochloride) (Standard) is the analytical standard of Octopamine (hydrochloride). This product is intended for research and analytical applications. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.

Propranolol (hydrochloride) (Standard) is the analytical standard of Propranolol (hydrochloride). This product is intended for research and analytical applications. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

1-Methoxy-2-propyl acetate is a volatile ester compound found in chocolate made from fermented cocoa beans. 1-Methoxy-2-propyl acetate serves as a hydrolysis substrate for esterases in blood, liver, lung, and nasal mucosa, and is rapidly hydrolyzed to propylene glycol monomethyl ether and acetic acid. 1-Methoxy-2-propyl acetate is proposed as a candidate urinary biomarker for dairy product intake. 1-Methoxy-2-propyl acetate can serve as a solvent and is applied in the electronic-grade semiconductor industry. 1-Methoxy-2-propyl acetate can be used in research related to nephropathy, hepatomegaly, and nasal irritation.

Butylboronic acid is a competitive soybean urease inhibitor with an IC₅₀ of 2.9 mM and a K_i of 1.5 mM.

Quinestrol (W-3566) is an orally effective synthetic estrogen compound that acts on CYP3A4, CYP1A2, and GnRH. Quinestrol interferes with GnRH release and disrupts the hypothalamic-pituitary-ovarian axis. Quinestrol downregulates the gene expression of follicle-stimulating hormone β and luteinizing hormone β, induces oxidative stress, damages reproductive organs, reduces sperm density and motility, increases sperm malformation rate, and alters the levels of sex hormones such as testosterone, luteinizing hormone, estradiol, and progesterone. Quinestrol can be used in studies related to reproductive function regulation.

CCX354 is an antagonist of CCR1, with anti-inflammatory activity.

Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I).

Maropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.

AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 to CXCR4, with IC₅₀s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC₅₀: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

XL228 is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a K_i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC₉₀s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).

Treprostinil palmitil is a long-acting inhaled pulmonary vasodilator prodrug of Treprostinil (HY-100441), formulated in a lipid nanoparticle (LNP). Treprostinil palmitil can inhibit pulmonary vascular remodeling induced by Su/Hx challenge in rats. Treprostinil palmitil can induce cough. Treprostinil palmitil demonstrates a sustained presence in the lungs with reduced systemic exposure and prolonged inhibition of hypoxia-induced pulmonary vasoconstriction in vivo. Treprostinil palmitil can be studied in research for pulmonary arterial hypertension and interstitial lung disease.

Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system.