Endocrinologie/Hormones

<p>FL442 is an Androgen Receptor (AR) modulator. This compound exhibits potent inhibitory effects in AR-dependent prostate cancer cells, showing similar suppression efficiency to the traditional antiandrogen drugs Bicalutamide and Enzalutamide. It also maintains antiandrogen activity against the Enzalutamide-resistant AR mutant F876L. The pharmacokinetic properties of FL442 in mice reveal a longer half-life (8 hours), excellent targeting (prostate tissue), and metabolic stability. Additionally, it is effective at inhibiting LNCaP tumor growth at low plasma concentrations (30 ng/mL).</p>

<p>LY2066948 is a selective oral estrogen receptor modulator (SERM) with high affinity for estrogen receptors ERα and ERβ (Ki of 0.51 and 1.36 nM, respectively) and displays potent anti-estrogenic activity. It effectively blocks the increase in uterine weight induced by ethinylestradiol in immature rats. LY2066948 is utilized in the research of uterine fibroids and myomas.</p>

BMS-986118 is a GPR40 full agonist targeting type II diabetes, prompting insulin release without hypoglycemia risk.

<p>(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist (K(i): cloned human ORL1=1.8 nM).</p>

<p>(+)-JJ-74-138 is a novel non-competitive androgen receptor (AR) antagonist capable of inhibiting enzalutamide-resistant castration-resistant prostate cancer (CRPC).</p>

<p>Compound NAP: MOR antagonist, crosses blood-brain barrier, EC50: 1.14 nM, Ki: 0.37 nM, useful for OUD research.</p>

TD-0212: Oral dual antagonist for AT1 (pKi 8.9) & NEP inhibitor (pIC50 9.2).

<p>GPR84 antagonist 1 is a highly selective, high-affinity competitive antagonist of human GPR84.</p>

<p>"MB-07344 sodium is a TR-β agonist with a 2.17 nM Ki, boosts Atorvastatin's cholesterol-lowering effects in various animals."</p>

<p>TD-0212 TFA is an oral AT1 receptor antagonist &amp; NEP inhibitor with pKi 8.9 &amp; pIC50 9.2.</p>

<p>Estrone acetate (Hogival) is an estrogen derivative and an activator of estrogen receptors (ER). This compound can enhance breast development, stimulate the secretion of pituitary prolactin, and induce both the proliferation and activation of lactotrophs, evidenced by the reduction in prolactin storage granule size and the increase in the volume density of the rough endoplasmic reticulum and Golgi apparatus. Estrone acetate holds potential for endocrinological research and for investigating the mechanisms by which estrogen influences pituitary function, prolactin regulation, and breast tumor models.</p>

EN171, a covalent ligand, selectively binds to C38 and C96 on 14-3-3, intensifying 14-3-3's interactions with ERα, YAP, and TAZ. This action impairs both estrogen receptor and Hippo pathway transcriptional activities. Beyond serving as a molecular glue to augment native protein interactions, EN171 also functions as a covalent recruiter for 14-3-3 in heterobifunctional molecules. This facilitates the sequestration of nuclear neo-substrates, such as BRD4 and BLC6, into the cytosol.

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

<p>ERα degrader 5 is an orally active, selective estrogen receptor (ER) reducer that acts on ERα (EC50: 1.1 nM). ERα degrader 5 shows anti-tumour effects in vivo.</p>

<p>ORIC-101 is a highly effective and selective glucocorticoid receptor antagonist (EC50: 5.6 nM). It also has anti-cancer activity.</p>

<p>κ opioid receptor antagonist</p>

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

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

<p>RX 809055AX is a long lasting opioid antagonist at mu and delta receptors.</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>SC13, a novel mitragynine analog, exhibits low-efficacy agonism at Mu opioid receptors and provides antinociception while minimizing adverse effects.</p>

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

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

<p>C108297: glucocorticoid modulator, combats diet obesity/inflammation, reduces appetite/lipid storage, boosts fat burn.</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>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>Amoitone B, a cystosporone B derivative, functions as an NR4A1 agonist and exhibits anticancer activity [1].</p>

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

L 365209 is an oxytocin antagonist.

<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>

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

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

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

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

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

<p>A4B17 is an inhibitor of androgen receptor N-terminal with potential for androgen-responsive prostate cancer treatment.</p>

<p>21-Deacetoxy deflazacort is a dehydrogenated derivative of Deflazacort, which is a glucocorticoid. As an inactive precursor, Deflazacort rapidly converts into the active metabolite, 21-Desacetyldeflazacort. This compound serves as both an anti-inflammatory and immunosuppressive agent.</p>

<p>ER degrader 10 (Compound 51) is an orally active estrogen receptor (ER) selective degrader and antagonist, with a DC50 of 0.43 nM and an IC50 of 0.56 nM. It inhibits the proliferation of ER-positive cells, with an IC50 ranging from 0 to 15 nM. ER degrader 10 exhibits weak inhibitory activity on the hERG channel, with an IC50 greater than 40 μM. It has blood-brain barrier permeability, with a brain/plasma ratio (Kp) of 3.05. In mouse models, ER degrader 10 demonstrates antitumor activity.</p>

<p>The pKi values of Allyphenyline oxalate (compound 9) for the α2-adrenergic receptor subtypes α2A, α2B, and α2C are 7.24, 6.47, and 7.07, respectively.</p>

<p>LEO 134310: Selective, non-steroidal GR agonist with 14 nM EC50, for topical skin disease treatment.</p>

<p>JNJ-1250132 is a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro.</p>

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

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

<p>(Rac)-Fidarestat ((Rac)-SNK 860) is the racemic form of Fidarestat, functioning as a potent inhibitor of the enzyme aldose reductase.</p>

<p>SJ1008066 is a MAGE-A11 inhibitor with an IC50 of 0.13 μM. It binds to the MAGE homology domain (MHD) and disrupts the MAGE-A11:PCF11 interaction.</p>

<p>GPR81 agonist 2 is a potent agonist targeting the GPR81 receptor, demonstrating EC50 values of 0.023 µM for hGPR81 and 0.123 µM for hGPR109A, respectively.</p>

<p>Compound EF2 (Androgen receptor antagonist 12) is an orally active antagonist of the androgen receptor (AR) with an IC50 of 0.30 µM. It inhibits the transcriptional activity of mutant AR and the proliferation of AR-positive PCa (prostate cancer) cell lines. Additionally, Compound EF2 blocks the nuclear translocation of AR and suppresses tumor growth in the C4-2B xenograft mouse model. This compound is used for research in prostate cancer.</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>Cort108297: selective GR modulator/antagonist, high GR affinity (Ki: 0.45nM), no other steroid receptor affinity.</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>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>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>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>

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

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

<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>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>Relacorilant is an oral glucocorticoid receptor antagonist with Ki of 7.2 nM, potential for treating Cushing's syndrome.</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>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>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>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>non-steroidal androgen receptor (AR) antagonist</p>

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

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

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

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

<p>SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.</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>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>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>Bromadoline is an opioid analgesic selective for the μ-opioid receptor.</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>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>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>ALS-I-41 is a novel, potent and selective antagonist of oxytocin receptor.</p>