Endocrinologie/Hormones

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

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

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.

Sunobinop (S 117957) is an opioid receptor-like orphan receptor (ORL1) modulator.

<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>

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

CCG258747 is a novel, selective inhibitor of the GRK2 subfamily.

<p>LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting cAMP production and activating CREB signaling, which results in antitumor activities like inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. It is applicable in research across various cancers, such as melanoma, pancreatic cancer, colorectal cancer, and lung cancer, as well as studies exploring the role of GPER in normal physiological and pathological processes.</p>

MK-6913 is a potent and selective agonist of estrogen receptor β.

<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>

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

<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>

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

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>A 74273, a nonpeptidic and renin inhibitor, may be used to treat cardiovascular diseases due to renin inhibition.</p>

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

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

<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>

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

<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.

<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>

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

22-Thiocyanatosalvinorin A (RB-64) is a potent selective agonist for the kappa-opioid receptor, exhibiting an EC50 value of 0.077 nM.

<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>

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

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

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

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>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>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>

<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>

<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>

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

<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.

BW 443C is a selective agonist of mu-opioid receptor.

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

<p>TUG-2181 is an antagonist of GPR84, with an IC50 value of 34 nM. It inhibits reactive oxygen species (ROS) production and IL-8 secretion induced by GPR84 agonists in human neutrophils. TUG-2181 is applicable for research in inflammation and fibrosis.</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.

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

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

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).

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

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.

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

GSK866 is a selective glucocorticoid receptor agonist (SEGRA).

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

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

<p>Cort108297: selective GR modulator/antagonist, high GR affinity (Ki: 0.45nM), no other steroid receptor affinity.</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>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>GSK5182 is a racemic mix of (E/Z) isomers, a selective ERRγ inverse agonist (IC50: 79 nM), and induces ROS in liver cancer.</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.

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

(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).

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

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>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>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>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>

non-steroidal androgen receptor (AR) antagonist

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

L-372662 is bioactive chemical.

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

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

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

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>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.