Endocrinology/Hormones

L 365209 is an oxytocin antagonist.

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

Emd 52297 is an inhibitor of renin.

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

MTI013 is a selective inhibitor of SARS-CoV-2 nsp14 Mtase (IC50: 2.98 µM) and an antiviral agent (IC50: 10.33 µM in HCoV-229E infected Huh7 cells). Additionally, MTI013 demonstrates synergistic antiviral effects when used in conjunction with the RdRp inhibitor SHEN26.

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

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

<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>

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.

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.

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

<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>

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

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

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

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.

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.

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.

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

Androgen receptor degrader-5 (compound 14k) demonstrates superior capabilities, specifically in androgen receptor degradation and antiproliferative activity, showcasing its promising properties.

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).

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.

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).

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

Isotodesnitazene is an opioid compound that primarily targets the μ-opioid receptor (MOR). It exhibits EC50 values of 34.8 nM and 142 nM for MOR-βarr2 and MOR-mini-Gi, respectively. Isotodesnitazene can be utilized for research in opioid drugs.

Anilopam is an opioid analgesic belonging to the benzazepine class and acts as an agonist at opioid receptors.

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.

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

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.

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.

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

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

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.

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

BMS-986034 is a GPR119 agonist.

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

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

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.

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

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

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

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.

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

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>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>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>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>

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].

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

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

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).

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

non-steroidal androgen receptor (AR) antagonist

L-372662 is bioactive chemical.

<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>

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

SR14150 is a partial agonist of high-affinity NOP receptor.

Bromadoline is an opioid analgesic selective for the μ-opioid receptor.

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<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.