(Des-Glu5)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production[1].
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE[1]. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[2].
Vemtoberant is an β3 Adrenergic Receptor antagonist. Vemtoberant can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure[1][2].
CO23 is a selective thyroid hormone receptor (TR) α agonist and used for growth and development regulation. CO23 was able to be transported through the blood-brain barrier[1].
MCHR1 antagonist 3 is a potent the melanin-concentrating hormone receptor-1 (MCHR1) antagonist. MCHR1 antagonist 3 is used to regulate energy metabolism[1].
CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. CRF1 receptor antagonist-1 can be used for research of congenital adrenal hyperplasia (CAH)[1].
ZD-7114 hydrochloride is a potent and selective agonist of β3-adrenergic. ZD-7114 hydrochloride is a selective thermogenic agent in vivo. ZD-7114 hydrochloride can be used in study obesity and diabetes[1].
Maysin, a neuroprotective C-glycosyl-flavone, can be isolated from corn silk. Maysinshows protective activity against the damage caused by Syn amyloid aggregates-oligomers and fibrils. Maysinprevents oxidative stress and imbalance of intracellular calcium homeostasis, activating an autophagic degradative process. Maysincan be used for research of Parkinson's disease (PD)[1].
GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone[1][2].
Propylthiouracil(6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor. Target: Thyroperoxidase (TPO)Propylthiouracil (PTU) is a thiouracil-derived drug used to treat hyperthyroidism (including Graves' disease) by decreasing the amount of thyroid hormone produced by the thyroid gland [1]. The antithyroid drug 6-propylthiouracil (PTU) was shown to have an unexpectedly prolonged inhibitory effect on iodination in the thyroid glands of rats. Eighteen hours after injection of a relatively small dose, iodination in the thyroid remained inhibited by more than 90% [2]. PTU inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin. This is one of the essential steps in the formation of thyroxine (T4). PTU does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors, such as perchlorate and thiocyanate. From Wikipedia.
Trioxifene mesylate (LY133314) is an antiestrogenic compound. Trioxifene mesylate elicits mixed agonist-antagonist actions on estrogen target tissues[1].
Fexofenadine-d10 (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years)[1].
Pindolol-d7 (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33 nM)[1][2].
Enclomiphene ((E)-Clomiphene) hydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene hydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1].
Plasma kallikrein-IN-1 is a PKK inhibitor with an IC50 value of 0.5 nM.
Cligosiban (PF-3274167) is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.IC50 value: 9.5 nM [1]Target: oxytocin receptor (OTR)
Retosiban (GSK221149A) is a potent and selective oxytocin antagonist with a Ki of 0.65 nM.
5a-Pregnane-3,20-dione is the endogenous progesterone metabolite.
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1].
Bisphenol B is a very close structural analog of Bisphenol A (HY-18260), an endocrine disrupting chemical (EDC) and a substance of very high concern (SVHC) in the European Union (EU) for both human health. Bisphenol B shows endocrine disruptive properties or other adverse effects on animal models[1].
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis[1].
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM)[1].
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity. Target: Androgen ReceptorCyproterone acetate clearly shows antagonistic properties, while being a partial agonist also, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations [1]. In the presence of 10 nM Testosterone, low concentrations of Cyproterone acetate inhibits T-stimulated transcription of 3XHRE-LUC, but at higher concentrations, transcription is stimulated. LH levels in Cyproterone acetate-treated rats do not dip below pretreatment levels, although they does not increase as much in the rats treated with 3.2 mg Cyproterone acetate/kg/day as in those which received 0.2 mg Cyproterone acetate/kg/day [2]. Cyproterone acetate exhibits direct negative effect on reproductive organs weight and significant reducing effect on sperm count and Ca2+ contents. SOD and GST activities significantly decrease in addition to significant increase in NO, MDA contents reflecting the oxidative status of testis in Cyproterone acetate treated rats [3].
pTH (13-34) (human) is apTH ((Human parathyroid hormone) fragment.
AT2 receptor agonist C21 is a druglike selective angiotensin II AT2 receptor agonist with Ki values of 0.4 nM and >10 µM for the AT2 receptor and AT1 receptor, respectively[1].
Novel serine hydroxymethyltransferase (SHMT) inhibitor, potently inhibiting both human SHMT1/2
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity[1][2].
LHRH, the luteinizing hormone-releasing hormone, is a neuropeptide hypothalamic. LHRH regulates reproduction. LHRH can be used for the research of cancer[1].
Carbimazole is an imidazole antithyroid agent. Target: OthersCarbimazole is an effective thyroid hormone inhibitor under a class of drugs known as pro-drugs. It is considered a pro-drug because it converts to methimazole after being absorbed by the body, generating an antithyroid action that works against hyperthyroidism (excessive production of thyroid hormones) and thyrotoxicosis (inflammation of the thyroid gland) [1]. Methimazole prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4 (thyroxine) [2].Carbimazole (CBZ) is one of the major drugs currently used for the treatment of Graves' disease. Experiments with [35S] CBZ in rats showed that the drug is so rapidly transformed to MMI after i.v. injection (within 3 min) that very little of the unchanged drug would be expected to reach the thyroid gland. The antithyroid action of CBZ in rats, therefore, can be ascribed entirely to the MMI to which it is rapidly converted [3].
Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].