Endocrinologie/Hormones

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).

BMS-986034 is a GPR119 agonist.

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

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.

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

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

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).

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.

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.

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.

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

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

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.

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.

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.

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).

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.

TD-0212 TFA is an oral AT1 receptor antagonist & NEP inhibitor with pKi 8.9 & pIC50 9.2.

AKR1C3-IN-5 inhibits AKR1C3, key in prostate/breast cancers, with MCF-7 cell IC50 of 9.6 μM.

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

U 80215 is an enzyme-competitive inhibitor.

5′-Guanidinonaltrindole (GNTI) is a selective antagonist of the kappa opioid receptor.

Saprisartan potassium is an Angiotensin II Type 1 receptor antagonist and antihypertensive agent.

Emd 52297 is an inhibitor of renin.

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.

NOP agonist-1 (compound 4) is a nociceptin opioid receptor (NOP) partial agonist that attenuates Parkinsonian disabilities in 6-OHDA hemilesioned rats [1].

Win 45164 is an orally active ligand for the glucocorticoid receptor (Glucocorticoid Receptor), exhibiting activity that inhibits the pituitary-adrenal axis. It enhances liver glycogen deposition and thymolysis in adrenalectomized male rats. Additionally, Win 45164 possesses anti-inflammatory properties and is applicable in research related to inflammation and neurological disorders.

Angiotensin AT2 receptor agonist

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.

δ receptor antagonist

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

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.

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

AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist that acts on wild-type AR (IC50: 246.6 nM).

Estrogen receptor-agonist-1 (compound 4e) is an estrogen receptor (ER) agonist that binds to ERα with high affinity.

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

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].

ERRγ agonist-1 can be used in neuropsychological disorders research.

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

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.

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

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

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).

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.

(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>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>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>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>

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

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

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

L-372662 is bioactive chemical.

non-steroidal androgen receptor (AR) antagonist

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].

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).

<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>

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

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

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

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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.