Endocrinologie/Hormones

KF-19418 is a follicle stimulant that directly activates follicles in vitro and promotes hair growth in vivo.

(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.

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

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.

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

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.

<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>

AP5 sodium: potent oral GPR40 agonist, enhances ligands, may aid type II diabetes research.

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

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.

<p>OT-R agonist 1 TFA (compound 5) is an oxytocin receptor (OT-R) agonist with an EC50 value of 0.39 nM. It exhibits V1A antagonist activity, with an EC50 value of 2432 nM, and can be utilized in studies related to central nervous system diseases.</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.

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.

Pentomone (LY-113935) is an anti-androgen compound that acts as a prostate growth inhibitor.

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

GSK866 is a selective glucocorticoid receptor agonist (SEGRA).

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

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.

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

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.

Estrogen receptor antagonist 4 blocks ER, impacting cell growth and cancer research potential.

ACT 178882 is a new Renin inhibitor (IC50: 1.4 nM).

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

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

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>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>

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

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

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

ERRα antagonist-2 is an estrogen-related receptor α inverse agonist, inhibiting migration and invasion in ER-negative MDA-MB-231,breast cancer.

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).

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

<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>

<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>

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.

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

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

<p>ERβagonist-1 (Compound 8) functions as a dual-active selective ERβ agonist (EC50: 46.8 nM) and an AR antagonist (IC50: 1555 nM). By binding to ERβ, it activates its signaling pathways while simultaneously inhibiting AR activity. Retaining selective ERβ agonist activity in mouse models, ERβagonist-1 is applicable in prostate cancer research.</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>

AR antagonist 11 (Compound c2) is a selective androgen receptor antagonist with an IC50 of 0.019 μM. It is also effective against the ARF877L/T878A mutant (IC50: 1.03 μM). Additionally, AR antagonist 11 inhibits LNCaP cell proliferation and decreases PSA protein expression (IC50: 0.54 μM). This compound is applicable in prostate cancer (PCa) research.

Fonsartan: Angiotensin receptor blocker, halts angiotensin II effects on rat vascular cells.

δ1 opioid receptor antagonist

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

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

Dynorphin A ethylamide (1-9), the opioid activities were examined in the bioassays.

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.

Compound 4x, also known as σ1 Receptor/μOpioid receptormodulator 2, acts as a μOR agonist and a σ1R antagonist, exhibiting a potent μOR EC50 of 0.6 nM and strong σ1R inhibitory activity (Ki: 363.7 nM). It demonstrates significant analgesic effects in various pain models.

OSU-ERb-12 is an ERβ agonist that suppresses ovarian cancer cell proliferation both in vitro and in vivo, and decreases the expression of Snail [1] [2].

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

<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>

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

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

Riminkefon is a kappa opioid receptor agonist .

<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>

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

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.

DS34942424 is an orally potent analgesic which did not exhibit mu opioid receptor agonist activity.

<p>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.</p>

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

<p>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.</p>

GPR84 antagonist 1 is a highly selective, high-affinity competitive antagonist of human GPR84.

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

Mepixetil is a potent angiotensin II receptor antagonist[1].

<p>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.</p>

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

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

<p>Bromadoline is an opioid compound that exhibits anti-nociceptive properties in rodents.</p>

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.

<p>Anticanceragent 257 (compound of formula (I)) is an anticancer agent that regulates Nur77 and Nurr1.</p>

5α-reductase-IN-1 is a potent inhibitor of the enzyme 5α-reductase.

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>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>

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

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

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

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

DS69910557: potent hPTHR1 antagonist, IC50 0.08 μM, oral, for hyperparathyroidism & osteoporosis research.

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.

RX 809055AX is a long lasting opioid antagonist at mu and delta receptors.

MLS000389544 is a selective and potent thyroid hormone receptor β (TRβ) antagonist with a methylsulfonyl nitrobenzoic acid structure. It effectively inhibits the interaction between TRβ and steroid receptor coactivator 2 (SRC2).

S-HP210: selective GR modulator, blocks NF-κB (IC50: 1.92 μM), non-toxic to mouse fibroblasts.

<p>CI 992 is a novel potent inhibitor of primate renin.</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>

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

<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>

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.

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.

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).

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.

ZK 216348 is a selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. also binds to progesterone receptors and mineralocorticoid receptors.

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

<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>

L-372662 is bioactive chemical.

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

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

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).

non-steroidal androgen receptor (AR) antagonist