Endocrinologie/Hormones

<p>κ opioid receptor antagonist</p>

<p>6β-Naltrexol is a peripherally selective opioid antagonist that reduces constipation from opioids while minimizing central nervous system effects.</p>

<p>RX 809055AX is a long lasting opioid antagonist at mu and delta receptors.</p>

J-113397 is a potent and selective NOP receptor antagonist (IC50 = 2.3 nM).

<p>PD 134922 is a HIV-1 protease inhibitors. Inactivation of the protease prevents infectious virion formation.</p>

<p>SB-612111 is a potent ORL-1 antagonist, with high affinity (Ki: 0.33 nM) and µ-receptor activity (Ki: 57.6 nM), blocking Nociceptin-induced pain.</p>

<p>Mopivabil is the angiotensin II receptor antagonist[1].</p>

<p>SC13, a novel mitragynine analog, exhibits low-efficacy agonism at Mu opioid receptors and provides antinociception while minimizing adverse effects.</p>

<p>Glucocorticoid Receptor Activator 1, a phenyl nitrogen-heterocyclic precursor, acts as an activator of the glucocorticoid receptor (GR). By activating GR, it downregulates the expression of pro-inflammatory genes stimulated by TNF, making it useful for inflammation research.</p>

BU09059 is a potent, selective, short-acting antagonist of the κ-opioid receptor (KOR).

<p>MK-6913 is a potent and selective agonist of estrogen receptor β.</p>

<p>BMS-986034 is a GPR119 agonist.</p>

<p>C108297: glucocorticoid modulator, combats diet obesity/inflammation, reduces appetite/lipid storage, boosts fat burn.</p>

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

<p>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).</p>

<p>ER antagonist 7, compound 13, inhibits ERs, halts breast/ovarian cancer cell growth, has anticancer properties.</p>

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

<p>EN1441 is a covalent degrader that targets the androgen receptor (AR) with an EC50 value of 4.2 μM, as well as its truncated variant AR-V7. It selectively and effectively degrades AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 holds potential for research into androgen-independent prostate cancer.</p>

<p>L162389 is an angiotensin II receptor antagonist with a balanced affinity for AT1 and AT2 receptor and stimulates the conversion of phosphatidylinositol.</p>

<p>AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist that acts on wild-type AR (IC50: 246.6 nM).</p>

<p>Estrogen receptor antagonist 6 is a potent blocker of estrogen signaling, regulating various biological effects. (Compound 166)</p>

<p>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.</p>

<p>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.</p>

JDTic Dihydrochloride is a high-affinity and selective κ-opioid receptor (KOR) antagonist that blocks dynorphin-KOR signalling,antidepressant.

<p>Amoitone B, a cystosporone B derivative, functions as an NR4A1 agonist and exhibits anticancer activity [1].</p>

<p>Metahexestrol is an inhibitor of the estrogen receptor (E2R) with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cell line with an ED50 of 1.0 μM. Additionally, Metahexestrol shows inhibitory activity in estrogen receptor-negative MDA-MB-231 cell lines, and its antiproliferative effect is not reversed by estrogen, suggesting that its mechanism may be partially independent of the E2R pathway. Metahexestrol is applicable in research on estrogen-dependent breast cancer.</p>

<p>22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcohol metabolite that exhibits both anti-progestational and anti-glucocorticoid activities. This compound contains an alkyne group and is capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Furthermore, 22-Hydroxy Mifepristone demonstrates a relative binding affinity of 48% to the human glucocorticoid receptor.</p>

L 365209 is an oxytocin antagonist.

<p>Potent, selective MOR antagonist (compound 26); crosses blood-brain barrier. Ki: 0.24 nM, EC50: 0.54 nM; for studying OUD.</p>

<p>Estrogen receptor antagonist 4 blocks ER, impacting cell growth and cancer research potential.</p>

<p>Muopioid Receptor Antagonist 8 (368) serves as an antagonist to the μ-opioid receptor, significantly inhibiting the activation of Gi induced by met-enkephalin at the µOR.</p>

Androgen receptor antagonist 11 (compound N29) is a selective, orally available antagonist.

<p>NSC 645827 is an inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1), with an IC50 of 0.7 μM.</p>

<p>(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.</p>

<p>Elacestrant (RAD1901) dihydrochloride, an oral ERR degrader, has IC50 of 48 nM (ERα) and 870 nM (ERβ). Its S enantiomer has low activity.</p>

<p>Naldemedine (S-297995) tosylate, a PAMORA, targets μ-, δ-, κ-opioid receptors, aiding OIC research, may bind to SARS-CoV2's 3CL pro.</p>

<p>AT1R antagonist 2 is a potent AT1R selective ligand with good AT1R affinity (Ki: 26 nM).</p>

<p>ID11916 is an orally active compound functioning as both an androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. It disrupts androgen binding to AR, impedes nuclear translocation, and blocks androgen-dependent transcriptional activity of AR, while simultaneously elevating intracellular cGMP levels by inhibiting PKG activation. Moreover, ID11916 exhibits potent anticancer effects in prostate cancer cell lines VCaP and 22Rv1, as well as in AR-positive breast cancer cell line SK-BR-3.</p>

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

<p>CH5447240: potent hPTHR1 agonist, treats Hypoparathyroidism, EC50 12 nM, 55% oral bioavailability, raises rat serum calcium.</p>

<p>SB-612111: potent ORL-1 antagonist, Ki=0.33 nM; μ-, κ-, δ-receptor Ki=57.6, 160.5, 2109 nM; blocks nociceptin's pain effect.</p>

<p>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).</p>

<p>JTP-117968: Non-steroidal SGRM, glucocorticoid receptor modulator, IC50 = 6.8 nM, offers better inhibitory/activatory balance.</p>

<p>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.</p>

<p>6:2 Cl-PFAES exhibits reproductive toxicity by elevating the levels of serum estradiol and vitellogenin in adult males, which can harm the embryonic development of offspring.</p>

<p>Glucocorticoid Receptoragonist-5 (compound 4) is an effective glucocorticoid molecule acting as a potent agonist for glucocorticoid receptors. It exhibits anti-inflammatory and immunosuppressive activities and serves as an ADC cytotoxin.</p>

<p>Compound 25: potent, selective MOR antagonist, crosses blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM), for OUD research.</p>

<p>Androstatrione is an androgenic compound.</p>

<p>Compound 31: Potent, selective MOR antagonist; crosses blood-brain barrier; Ki &amp; EC50: 0.38 nM; useful for OUD research.</p>

<p>ERRγ agonist-1 can be used in neuropsychological disorders research.</p>

<p>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.</p>

<p>BU72 is a potent, long-lasting agonist for μ and κ opioid receptors, with partial agonistic activity at the δ opioid receptor (EC50 values of 0.054, 0.033, and 0.58 nM, respectively). It provides strong, enduring analgesic effects primarily mediated through μ opioid receptors. BU72 also exhibits a prolonged duration of activity and can partially reverse morphine-induced analgesia. It is applicable in studies of opioid dependence.</p>

<p>Mepixetil is a potent angiotensin II receptor antagonist[1].</p>

<p>AP5: GPR40 agonist, positive allosteric modulator; rat hIP1 EC50: 0.49 nM.</p>

<p>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>

<p>KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. When labeled with the 11C isotope, KR31173 can be used as a tracer for positron emission tomography (PET). In mice, KR31173 exhibits favorable biodistribution and pharmacological characteristics. It selectively binds to organs in CD-1 mice known to have a high density of AT1 angiotensin receptors.</p>

<p>AVE 0991 is a nonpeptide analog of angiotensin-(1-7), a Mas agonist with inhibitory effects on [125I]-Ang-(1-7) and on neuroinflammation in Alzheimer's disease.</p>

<p>KNT-127 is an agonist of δ-Opioid receptor.</p>

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

<p>ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.</p>

<p>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.</p>

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

<p>Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used in the study of opioid overdose and alcohol dependence.</p>

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

<p>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.</p>

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

<p>ZK 216348 also binds to Progesterone and mineralocorticoid receptors (IC50s: 20.4 nM and 79.9 nM, respectively). ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist (IC50: 20.3 nM). ZK 216348 has an anti-inflammatory activity similar to</p>

<p>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.</p>

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

<p>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>

<p>Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.</p>

<p>Budesonide (Pulmicort), an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.</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>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>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>

<p>non-steroidal androgen receptor (AR) antagonist</p>

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

<p>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].</p>

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

<p>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).</p>

<p>Erb-196 is an estrogen receptor-receptor agonist with non-steroidal selectivity.</p>

<p>L-372662 is bioactive chemical.</p>

<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>YK11 is an androgen receptor partial agonist that activates androgen receptor transcriptional activity in HEK293 cells overexpressing androgen receptors when used at a concentration of 0.1 μM, with osteogenic activity.</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>SR14150 is a partial agonist of high-affinity NOP receptor.</p>

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

<p>Bromadoline is an opioid analgesic selective for the μ-opioid receptor.</p>

<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>

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