Fluticasone is an inhaled corticosteroid used for respiratory diseases[1]. Fluticasone is a Smo agonist s with a IC50 value of 99 nM. Fluticasone activate Hedgehog signaling and promotes the proliferation of primary neuronal stem/precursor cells[2].
ONO-0300302 (ONO0300302) is a novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM; shows excellent in vivo efficacy, represents a best research tool available to LPA-related diseases.
Trh-gly (TRH-glycine) is a precursor of thyrotropin (TSH)-releasing hormone (TRH) that can release thyrotropin and prolactin[1].
Hydroflumethiazide (Methforylthiazidine) is an orally active and potent thiazide diuretic. Hydroflumethiazide possesses the ability to directly stimulate A cell secretion in the normal and alloxan diabetic pancreas[1][2][3].
Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity[1][2]. Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanoma cells[2].
Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
Aganepag isopropyl (AGN-210961) is an EP2 agonist[1][2].
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory[1][2].
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 µM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation [1][2][3].
Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis[1][2].
Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion[1][2].
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR)[1].
Dienestrol-d2 is a deuterium labeled Dienestrol (HY-B1403).
LY88074 Methyl ether (Example 2) is useful for the inhibition of the various estrogen deficient conditions, which are associated with estrogendeprivation syndrome including osteoporosis and hyperlipidemia[1].
Diethylstilbestrol-d3 is deuterium labeled Diethylstilbestrol.
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy[1][2].
13-cis-Retinyl acetate (13-cis-Retinol acetate; 13-cis-Vitamin A acetate) is a 13-cis isomer formed by Retinyl acetate. 13-cis-Retinyl acetate is an active metabolite of vitamin A[1].
Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms[1][2].
Macimorelin (EP-1572), a GH secretagogue, is an orally active GHSR agonist. Macimorelin stimulates GH release. Macimorelin can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS)[1][2][3].
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
Metaproterenol (Orciprenaline) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol also has anti-inflammatory activity[1][2].
RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). IC50 value: 7 nM (Ki, fot androgen receptor) [1]Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM). [1] RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.[2]in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys. [1] RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.[2]
Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research[1].
Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. Methylergometrine can be used as oxytocin and has protective effect on postpartum hemorrhage[1][2][3].
Mating Factor α (1-6) is a mating factor produced by α-mating type cells of Saccharomyces cerevisiae and an acts as an inhibitor of the initiation of DNA synthesis in the cells[1].
Butaxamine (Butoxamin) hydrochloride is a specific β2-adrenergic receptor blocker. Butaxamine hydrochloride inhibits the decreases in urine volume in ethanol-anesthetized, water-diuretic rats[1].
(Rac)-Dobutamine-d4 hydrochloride is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
Makisterone A, a 28-carbon moulting hormone, has been identified as the major free pupal ecdysteroid in the honey bee, Apis mellifera[1].
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.