Endocrinology/Hormones

CI 992 is a novel potent inhibitor of primate renin.

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.

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

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).

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

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.

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

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).

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

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

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

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

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.

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.

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.

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

δ receptor antagonist

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

Emd 52297 is an inhibitor of renin.

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

U 80215 is an enzyme-competitive inhibitor.

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

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

Angiotensin AT2 receptor agonist

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.

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

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.

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.

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

TRβ Agonist 1, a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, demonstrates an EC50 value of 21 nM.

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.

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.

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

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

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

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

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.

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.

(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).

<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>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>

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).

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

L-372662 is bioactive chemical.

non-steroidal androgen receptor (AR) antagonist

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].

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>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>Gastric inhibitory polypeptide (GIP) is an inhibiting hormone of the secretin family of hormones. While GIP is a weak inhibitor of gastric acid secretion, its main role is to stimulate insulin secretion - in a glucose-dependent mechanism. Therefore, GIP is referred to as a glucose-dependent insulinotropic peptide. In GIP (Pro 3) the glutamic acid at position 3 has been substituted for a proline.GIP is derived from a 153-amino acid proprotein encoded by the GIP gene and circulates as a biologically active 42-amino acid peptide. It is synthesised by K cells, which are found in the mucosa of the duodenum and the jejunum of the gastrointestinal tract. GIP receptors are seven-transmembrane proteins found on β-cells in the pancreas. These β-cells are those that are able to simultaneously detect glucose and release insulin as a result to GIP binding.The clinical relevance of GIP is related to type 2 diabetes mellitus (T2DM)- studies have found that T2DM diabetics are unresponsive to GIP and have lower levels of GIP secretion after a meal when compared to non-diabetics. In research involving knockout mice, it was found that absence of the GIP receptors correlates with resistance to obesity.</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>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>

<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>

ALS-I-41 is a novel, potent and selective antagonist of oxytocin receptor.