Endocrinologie/Hormones

<p>Aldose reductase-IN-2 (5f) inhibits AR with antioxidant effects; potential anti-diabetic drug.</p>

<p>Zuclomiphene is a nonsteroidal selective estrogen receptor modulator (SERM) with triphenylethylene group.</p>

<p>SIM-688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).</p>

<p>ASN06917370 (Compound V) is a specific modulator of the orphan receptor GPR17 (Uracil Nucleotide/Cysteinyl Leukotriene Receptor), neuroprotective</p>

<p>AZ12216052 is a GRP8 antagonist with anxiolytic and anti-inflammatory activity and can be used to study obesity and metabolic disorders.</p>

<p>ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist (IC 50=40 nM) [1].</p>

L-751788 is an inhibits of type 1 5alpha-reductase.

<p>Olmesartan methyl ester: an intermediate for synthesizing Olmesartan medoxomil, a strong AT1 receptor blocker.</p>

<p>AR inhibitor Aldose reductase-IN-6: IC50 3.164 μM, Ki 0.018 μM, non-toxic to normal cells.</p>

<p>Aldose reductase-IN-4 (compund IIc) is an inhibitor of aldose reductase with IC50s of 11.70 μM and 0.98 μM for ALR1 and ALR2, respectively [1].</p>

<p>L-366,509 is an antagonist of oxytocin.</p>

<p>Endomorphin 1 acetate is a μ-opioid receptor agonist with antinociceptive and analgesic effects and can be used to study neurological diseases.</p>

<p>Cyprodinil is a fungicide blocking methionine synthesis in fungi and hinders B. cinerea, P. herpotrichoides, H. oryzae growth; it's also an AR agonist.</p>

<p>HG122 promotes AR degradation via proteasome, inhibiting castration-resistant prostate cancer.</p>

<p>Idoxifene is a tissue-specific selective estrogen receptor modulator.</p>

<p>Camizestrant (Estrogen receptor antagonist 2) is an antagonist of the estrogen receptor and can be used in studies about ER+ HER2-advanced breast cancer[1].</p>

<p>Potent, selective oral GPR84 antagonist with IC50 of 8.95 nM, inhibits neutrophil/macrophage chemotaxis, potential in ulcerative colitis research.</p>

<p>LY 281217, an organic opioid agonist, can produce analgesic effects in mice.</p>

<p>Dehydro Olmesartan, from Olmesartan, is an AT1R blocker for researching hypertension.</p>

ERβ receptor agonist

<p>Chlorothalonil (DAC 2787): Broad-spectrum, efficient, low-toxicity fungicide for fruits, vegetables, rice, wheat, cotton.</p>

<p>LY285434 is a suitable angiotensin II receptor antagonist.</p>

<p>Desketoraloxifene is a selective estrogen receptor modulator, inhibiting mammalian PLD (PLD1 and PLD2).</p>

<p>agonist at ERα receptor and antagonist at ERβ receptor</p>

<p>Dimethomorph is a fungicide and sterol biosynthesis inhibitor that inhibits fungal cell wall formation,. inhibits androgen receptor (AR) .</p>

<p>PF-4455242 HCl is a selective and orally available κ-opioid receptor antagonist that exhibiting antidepressant effects.</p>

<p>Org-34517, a glucocorticoid receptor (GR) antagonist, is used potentially for the treatment of depression.</p>

<p>Capesaris (GTX-758) is an oral estrogen receptor α agonist, used in prostate cancer research.</p>

<p>GW7604 is an antiestrogen and it also is the metabolite of GW5638. GW5638 is an antagonist of high-affinity estrogen receptor (ER).</p>

<p>L-162,313 is an ANG II receptor agonist, a nonpeptide that mimics the biological actions of angiotensin II and induces an increase in MAP.</p>

<p>CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.</p>

PSB-CB5 (GPR18-IN-32)2 is a GRP18 antagonist with anti-inflammatory activity and can be used to study obesity and metabolic disorders.

<p>Estrogen Receptor Antagonist 8 is an ER antagonist with anti-uterine activity and may be used in the study of ovarian dysfunction.CASNETIN SODIUM (CasN)</p>

<p>AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively).</p>

<p>Endoxifen HCl, a Tamoxifen metabolite, targets estrogen receptors more effectively and blocks aromatase, showing promise for breast cancer research.</p>

<p>Faxeladol: adrenergic, serotonin inhibitor &amp; opioid agonist for neurological studies.</p>

ML-335, a μ-δ targeted agonist and MOR/DOR ligand, may lead to isomer-biased drugs with pain-relief properties.

<p>Moveltipril (Moveltipril calcium) is a potent angiotensin-converting enzyme (ACE) inhibitor.Moveltipril is converted to captopril in the body for action.</p>

<p>P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R (IC50: 3.17 μM) and GPR17 (IC50: 1.67 μM) antagonist.</p>

<p>Trimebutine CTB salt (GIC-1001) is an opioid receptor agonist used in the study of pain.</p>

<p>Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].</p>

<p>AMG-009 is a prostaglandin D2 antagonist. For CRTH2 and DP receptors, the IC50s are 3 nM and 12 nM, respectively.</p>

<p>G36 is a cell-permeable non-steroidal antagonist of GPER.</p>

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<p>GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity.</p>

<p>FPL-62129 is a calcium channel antagonist and a novel angiotensin-converting enzyme inhibitor with vasodilator activity for the study of cardiovascular disease.</p>

<p>Indazole-Cl is a selective ERß agonist and a selective estrogen receptor modifier (SERM).</p>

<p>SB-657510: UT antagonist, Ki (nM) - human 61, monkey 17, cat 30, rat 65, mouse 56; reduces UII-induced inflammation, aids diabetic atherosclerosis.</p>

<p>AZD9567: potent, selective SGRM, oral, IC50=3.8nM, effective in SCW joint inflammation.</p>

<p>ICI 199,441 hydrochloride is a potent, selective agonist of κ-opioid receptor.</p>