Endocrinology/Hormones

ERα degrader11 (compound B16) is a selective estrogen receptor degrader designed for use as a probe in examining the ER status within ER-positive breast cancer cells.

AR antagonist 10 (Compound Y5) is a potent, orally active androgen receptor (AR) antagonist with an IC50 value of 0.04 μM. It demonstrates a dual mechanism of action: antagonizing AR by disrupting AR dimerization and inducing AR degradation through the ubiquitin-proteasome pathway. This compound shows excellent activity against various resistant AR mutants and effectively inhibits the growth of LNCaP xenograft tumors. AR antagonist 10 is applicable for research in resistant prostate cancer.

PBPE hydrochloride is a derivative of tamoxifen and functions as a selective ligand for antiestrogen binding sites (AEBS). The binding affinity (Ki) of PBPE hydrochloride and MBPE to AEBS is 8.79 nM and 17.57 nM, respectively.

Estrogen receptor modulator11 (Compound 27) is a tetrahydroisoquinoline derivative. It exhibits affinity for the estrogen receptor (ER), with IC50 values of 285 nM for ERα and 421 nM for ERβ. Estrogen receptor modulator11 does not demonstrate antagonist activity in MCF-7 cell assays.

Norbinaltorphimine dihydrochloride is a selective and potent κ opioid receptor antagonist that induces itch-associated responses in mice.

Bromadoline is an opioid compound that exhibits anti-nociceptive properties in rodents.

Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression and exhibits anti-estrogenic activity by suppressing Estradiol-induced proliferation of MCF-7 cells, with an EC50 of 341 μM. Additionally, Triisopropyl phosphate reduces estrogen response element (ERE)-stimulated luciferase activity in MVLN cells, with an EC50 of 900 μM.

GW856464 is an antagonist of MCHR1. It is utilized in research related to cardiovascular diseases and obesity.

Androgen receptorligand 1 is a ligand for the androgen receptor (AR). It interacts with the CRBN E3 ligase via a linker to form an AR-PROTAC degrader. This compound is useful in prostate cancer research.

(S)-MCOPPB is the S-enantiomer of MCOPPB, an orally active selective agonist for the Nociceptin/Orphanin FQ-Receptor. It inhibits signal transduction in mouse brain NOP receptors and is utilized in anxiety disorder research.

KNT-127 is an agonist of δ-Opioid receptor.

AP5: GPR40 agonist, positive allosteric modulator; rat hIP1 EC50: 0.49 nM.

Naltrindole 5′-isothiocyanate (5'-NTII) is an irreversible delta opioid receptor antagonist that counters the analgesic effects induced by DSLET without altering the effects caused by DPDPE.

GSK866 is a selective glucocorticoid receptor agonist (SEGRA).

Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM).

<p>Opioid receptor antagonist 1 (Compound 10) is an Orvinol-based antagonist of opioid receptors. It exhibits activity as an antagonist against the analgesic properties of morphine.</p>

AKR1C3-IN-8 (Compound 5) is an effective and selective AKR1C3 inhibitor (IC50=0.069 μM). AKR1C3-IN-8 has antitumor activity.

Erα-IN-1 (compound 3c) is an inhibitor of the estrogen receptor α (ERα), effectively blocking ERα activity in MCF7/ERE-LUC cells.

PROTACAndrogen receptor degrader-1 (Ex.14) is a PROTAC degrader targeting the androgen receptor, with a DC50 of 6 nM. This compound is applicable in prostate cancer research.

Salvinorin A propionate: partial KOR agonist, Ki=32.6 nM, EC50=4.7 nM; ignores μ/δ/ORL-1, non-opioid receptors; less potent analgesic vs. salvinorin A.

Emd 52297 is an inhibitor of renin.

Galaxolide can induce estrogenic activity (Estrogen Receptor/ERR), oxidative stress, and genotoxicity. It also stimulates the enzymatic activities of EROD and GST (Glutathione S-transferase).

LIT-001, a nonpeptide OT-R agonist, enhances mouse autism-like behavior, with EC50=55 nM and Ki=226 nM.

GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, a novel selective androgen receptor modulator.

Androgen receptor degrader-5 (compound 14k) demonstrates superior capabilities, specifically in androgen receptor degradation and antiproliferative activity, showcasing its promising properties.

BMS-986034 is a GPR119 agonist.

ADX61623 is an effective negative allosteric modulator (NAM) of the follicle-stimulating hormone receptor (FSHR). It also exhibits activity on the luteinizing hormone receptor (LH-R) but is inactive on the thyroid-stimulating hormone (TSH) receptor. ADX61623 can be utilized in research on estrogen-dependent diseases.

5α-Tetrahydrocorticosterone (5α-HB) is an endogenous steroid that acts as an agonist of the glucocorticoid receptor (GR) and a metabolite of corticosterone. It serves as an effective topical anti-inflammatory agent in vivo. In rat liver cells, it decreases the binding of metabolites to the glucocorticoid receptor-corticosterone and its 5α-reduced metabolites, with a Kd value of 268 nM. 5α-Tetrahydrocorticosterone is applicable in research on inflammatory skin diseases.

GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 200 nM and 35 nM for hTRα and hTRβ, respectively.

Sob-AM2 is an effective substrate targeting the fatty acid amide hydrolase (FAAH) expressed in the brain, with a Km of 1.3 μM. It delivers higher concentrations of Sobetirome to the central nervous system at minimal peripheral systemic doses, thereby activating the central thyroid hormone receptor β (TRβ).

Angiotensin AT2 receptor agonist

FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s) protein-coupled human follicle-stimulating hormone (FSH) receptor. It exhibits an IC50 value of 28 nM in cell lines expressing the human FSH receptor. This compound significantly inhibits follicle growth and ovulation in in vitro mouse models.

Androgen receptor antagonist 13 (compound 8a) is an orally active androgen receptor antagonist with an IC50 of 0.20 μM. It is used in prostate cancer research.

5′-Guanidinonaltrindole (GNTI) is a selective antagonist of the kappa opioid receptor.

RJG-2051 is a selective covalent inhibitor of aldo-keto reductase family 1 member C3 (AKR1C3), with an IC50 value of 13 nM. It interferes with the metabolism of substrates such as androgens, estrogens, and prostaglandins through AKR1C3. RJG-2051 holds potential for cancer research.

Ciprokiren, a renin inhibitor by Roche, halts human renin; IC50: 0.07/0.65 nmol/L. Lowers blood pressure in animals. Preclinical development ceased.

(E/Z)-OT-R antagonist 1 is a mixture of the E/Z configurations of OT-R antagonist 1. This compound is a novel, potent, selective, non-peptide OT-R antagonist that inhibits oxytocin-induced intracellular Ca2+ activity with an IC50 of 8 nM.

ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.

Cort108297: selective GR modulator/antagonist, high GR affinity (Ki: 0.45nM), no other steroid receptor affinity.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.

GSK5182 is a racemic mix of (E/Z) isomers, a selective ERRγ inverse agonist (IC50: 79 nM), and induces ROS in liver cancer.

LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.

Mapracorat (ZK-245186, BOL-303242X) is a selective glucocorticoid receptor agonist,anti-inflammatory agent for atopic dermatitis and allergic conjunctivitis.

ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35.

(S)-Mapracorat is a selective and less active agonist of the glucocorticoid receptor.

PSN632408 is an optimized agonist of GPR119 receptors that display similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50: 5.6 and 7.9 uM, respectively).

<p>The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat VLDL. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat VLDL. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Rat VLDL, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat VLDL in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

<p>The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Horse IGF1. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Horse IGF1. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Horse IGF1, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Horse IGF1 in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

<p>Relacorilant is an oral glucocorticoid receptor antagonist with Ki of 7.2 nM, potential for treating Cushing's syndrome.</p>

<p>This assay employs the competitive inhibition enzyme immunoassay technique. The microtiter plate provided in this kit has been pre-coated with Mouse MDA protein. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Mouse MDA. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Mouse MDA in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

Erb-196 is an estrogen receptor-receptor agonist with non-steroidal selectivity.

non-steroidal androgen receptor (AR) antagonist

Omzotirome (TRC150094) is a functional analog of iodothyronines and holds potential for research on hyperlipidemia (WO2008149379).

21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione is a valuable organic compound for life sciences research [Catalog No.: T67476, CAS No.: 37413-91-5].

AZD9496 maleate is a highly potent and selective antagonist of the estrogen receptor alpha (ERα), exhibiting an IC50 value of 0.28 nM. This compound, AZD9496 maleate, is an orally bioavailable selective estrogen receptor degrader (SERD).

L-372662 is bioactive chemical.

Phosphoramidon Disodium (Phosphoramidon Disodium Salt) Salt is a metalloendopeptidase inhibitor, widely used as a biochemical tool.

Compound 5, a selective GPR109a agonist, exhibits a pEC50 value of 5.53 [1].

<p>SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.</p>

<p>Cebranopadol (GRT6005) is an analgesic NOP and opioid receptor agonist with Kis of 0.9 nM, 0.7 nM, 2.6 nM, 18 nM for human NOP, μ-opioid (MOP), κ-opioid (KOP)</p>

<p>Pamoic acid is the orphan G protein-coupled receptor GPR35 agonist. Pamoic acid activates ERK and beta-arrestin2 and causes antinociceptive activity.</p>

<p>This 32 amino acid peptide contains a 17 amino acid ring structure that is common to all natriuretic peptides. It is also called the brain natriuretic peptide (BNP) because it was first identified in porcine brain- however, the main source of this peptide is not the brain but the cardiac ventricle. This cardiac neurohormone is secreted from the ventricles in response to volume expansion and pressure overload. It has natriuretic and vasodilatory effects and suppresses the renin-angiotensin-aldosterone system.</p>

<p>Gastric inhibitory polypeptide (GIP) is an inhibiting hormone of the secretin family of hormones. While GIP is a weak inhibitor of gastric acid secretion, its main role is to stimulate insulin secretion - in a glucose-dependent mechanism. Therefore, GIP is referred to as a glucose-dependent insulinotropic peptide. In GIP (Pro 3) the glutamic acid at position 3 has been substituted for a proline.GIP is derived from a 153-amino acid proprotein encoded by the GIP gene and circulates as a biologically active 42-amino acid peptide. It is synthesised by K cells, which are found in the mucosa of the duodenum and the jejunum of the gastrointestinal tract. GIP receptors are seven-transmembrane proteins found on β-cells in the pancreas. These β-cells are those that are able to simultaneously detect glucose and release insulin as a result to GIP binding.The clinical relevance of GIP is related to type 2 diabetes mellitus (T2DM)- studies have found that T2DM diabetics are unresponsive to GIP and have lower levels of GIP secretion after a meal when compared to non-diabetics. In research involving knockout mice, it was found that absence of the GIP receptors correlates with resistance to obesity.</p>

SR14150 is a partial agonist of high-affinity NOP receptor.

Bromadoline is an opioid analgesic selective for the μ-opioid receptor.

Ceronapril (SQ 29852) is an orally active and potent angiotensin-converting enzyme (ACE) inhibitor (IC50 : 36 nM) for the study of dementia and hypertension.

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<p>Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells</p>

<p>MOR Agonist-1 is a μ-opioid receptor (MOR) agonist noted for its potent analgesic properties and is utilized in research concerning pain and associated</p>

ALS-I-41 is a novel, potent and selective antagonist of oxytocin receptor.