Endocrinologie/Hormones

<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.</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>Mepixetil is a potent angiotensin II receptor antagonist[1].</p>

<p>AP5: GPR40 agonist, positive allosteric modulator; rat hIP1 EC50: 0.49 nM.</p>

<p>Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM).</p>

<p>KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. When labeled with the 11C isotope, KR31173 can be used as a tracer for positron emission tomography (PET). In mice, KR31173 exhibits favorable biodistribution and pharmacological characteristics. It selectively binds to organs in CD-1 mice known to have a high density of AT1 angiotensin receptors.</p>

<p>AVE 0991 is a nonpeptide analog of angiotensin-(1-7), a Mas agonist with inhibitory effects on [125I]-Ang-(1-7) and on neuroinflammation in Alzheimer's disease.</p>

<p>KNT-127 is an agonist of δ-Opioid receptor.</p>

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

<p>ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.</p>

<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>

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

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

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

<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>Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.</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>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>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>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>non-steroidal androgen receptor (AR) antagonist</p>

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

<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>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>

<p>Erb-196 is an estrogen receptor-receptor agonist with non-steroidal selectivity.</p>

<p>L-372662 is bioactive chemical.</p>

<p>SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.</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>Pamoic acid is the orphan G protein-coupled receptor GPR35 agonist. Pamoic acid activates ERK and beta-arrestin2 and causes antinociceptive activity.</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>Bromadoline is an opioid analgesic selective for the μ-opioid receptor.</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>

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