Endocrinology/Hormones

<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>

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

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

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

Dazucorilant (CORT113176), a selective non-steroidal GR modulator, has high affinity with a K i <1 nM, useful for neurological research.

<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>

<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>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>

GDC-0927 Racemate is a degrader of estrogen receptor, is used in the research of ER-related diseases, potently inhibits ER-α activity, with an IC50 of 0.2 nM.

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

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

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

κ opioid receptor antagonist

<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>

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

AR ligand-44 is an androgen receptor (androgen receptor) ligand that can be utilized in the synthesis of PROTACs such as [ARD-2051].

AKR1C3-IN-7 (Compound 13) is an effective and selective AKR1C3 inhibitor (IC50=0.19 μM). AKR1C3-IN-7 has antitumor activity.

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

L 365209 is an oxytocin antagonist.

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

ErSO-DFP activates a-UPR, targets ERα+ cancer cells with high selectivity, and effectively reduces MCF-7 tumours.

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

Phenethyl 4-ANPP is a MOR (μ-opioid receptor) agonist with a structure similar to known opioids.

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

<p>Riminkefon is a kappa opioid receptor agonist .</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>

LXT34 (Example 2) is a GPR120 agonist with anti-inflammatory properties. This compound enhances GLP-1 formation in the gastrointestinal tract and improves insulin resistance in macrophages and pancreatic cells. LXT34 is applicable in studies related to inflammatory conditions, such as type 2 diabetes, obesity, and non-alcoholic fatty liver disease.

THR-β agonist 4 is a potent agonist of THR-β.

<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>

THR-β agonist 5 (compound 54) is a potent THR-β agonist, with an EC 50 of <50 nM [1].

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>GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.</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>ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.</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>

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

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

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

<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>

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>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>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>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>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>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.