Endocrinologie/Hormones

<p>Pratosartan is a selective antagonist of angiotensin II receptor.</p>

<p>L 158338 is an antagonist of the angiotensin receptor.</p>

<p>RU 58642 is an effective systemic antiandrogen for androgen-dependent disorders.</p>

<p>Paraprost consists of 1-glutamic acid, alanine, and glycine. It was used in prostate hypertrophy drug therapy.</p>

<p>TPBM inhibits ERα, non-toxic, blocks E2-ERα gene binding, halts ERα+ cancer cell growth (IC50: 5-9 μM), no effect on estrogen-independent growth.</p>

<p>Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide with affinity for the glucocorticoid receptor. a glucocorticoid with anti-inflammatory.</p>

<p>GPR40 Activator 2 is a highly effective activator of the GPR40 receptor.</p>

<p>SQ 31844 is a representative of the imidazole alcohols-a novel class of renin inhibitors.</p>

<p>UR-7247 is an angiotensin type 1 receptor antagonist with a very long plasma elimination half-life.</p>

<p>MK319 is an AKR1B10 inhibitor.</p>

<p>ML 190 is a potent and selective κ opioid receptor (KOR) antagonist (Ki=129 nM), exhibiting an IC50=150 nM in β-arrestin assays, drug addiction.</p>

<p>Dunnione is an antifungal agent exerting its action primarily through initiation of redox cycling.</p>

L 156373 is an oxytocin antagonist.

<p>GW5638, a prodrug of GW7604, is a unique estrogen receptor antagonist &amp; a pseudo-SERD with potential in breast cancer therapy.</p>

<p>SB-436811 is an antagonist of human urotensin-II receptor.</p>

<p>Ici 174865 is a delta opioid receptor antagonist agent.</p>

<p>Isoflupredone, a synthetic corticosteroid, inhibits inflammation and immune response in animals.</p>

<p>LY 164929 is a highly selective ligand for the lower affinity [3H]D-Ala2-D-Leu-5-enkephalin binding site.</p>

<p>FR 62765 is a derivative of WF-3681, an aldose reductase inhibitor.</p>

<p>Paramethasone Acetate is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive effects that can be used in the treatment of systemic lupus</p>

<p>D 15413 is an inhibitor of estrogen-dependent mammary tumors.</p>

<p>MK204 is an inhibitor of AKR1B10, a tumor marker and promising antineoplastic target.</p>

<p>Iodothiouracil is a uracil derivative. It was used as a thyroid antagonist.</p>

(Rac)-ErSO-DFP, an ErSO-DFP derivative, modulates ERα, targets ERα+ breast cancer & resistant tumors (from patent WO2022087234A1).

<p>Levormeloxifene fumarate is an osteoporosis drug and selective estrogen receptor modulator (SERM).</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>Palatrigine (BW-A 256C) is a compound with angiotensin-converting enzyme inhibitory and beta-adrenergic receptor blocking properties.</p>

<p>Estredox, an estrogen receptor agonist, is used potentially for the treatment of vasomotor symptoms.</p>

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

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Minalrestat(ARI-509) is an orally active and potent aldose reductase inhibitor for the study of impaired microvascular reactivity in diabetic patients.

<p>Y134, an oral estrogen receptor inhibitor, is 121x more selective for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM), and blocks ER+ breast cancer cell growth.</p>

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

<p>Finrozole (MPV 2213ad) is a novel selective aromatase inhibitor that is partially reversible for breast development.</p>

<p>GLPG0492 is a novel selective androgen receptor modulator.</p>

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

<p>LY2881835 is a potent and selective GPR40 agonist.</p>

<p>GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM,</p>

<p>ADL-5747 (ADL-5747 (free base)) (free base) is a delta opioid receptor agonist used in the treatment of neurological disorders, skin and musculoskeletal</p>

<p>MEDICA16: GPR40 agonist, GPR120 partial agonist, ATP-citrate lyase inhibitor, lowers TG, boosts insulin sensitivity in muscle.</p>

<p>Bevenopran (CB-5945) is a peripheral antagonist of μ-opioid receptor and can be used in studies about the treatment of opioid-induced bowel dysfunction.</p>

<p>Lorundrostat is an aldosterone synthase inhibitor.</p>

<p>YL-365 is a highly potent and selective GPR34 antagonist that exhibits excellent activity in neuropathic pain models for the study of neurologic diseases.</p>

MK 1903 is a strong, selective HCA2/GPR109A agonist, reducing cAMP in CHO cells with EC50 of 12.9 nM.

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

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

<p>FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.</p>

<p>ATC 0175 hydrochloride is an orally active melanocyte concentrating hormone 1 receptor antagonist that is potent and selective.</p>

<p>LP-471756 is a specific antagonist of GPR139 and inhibits LP-360924-stimulated cAMP production (IC50 = 640 nM).</p>

<p>SSR126768A is an oxytocin receptor antagonist that inhibits uterine contractions and may be used to prevent preterm labor.</p>

<p>Acifran (AY 25712) is an HM74A/GPR109A and GPR109B agonist and displays antihyperlipidemic activity.</p>

<p>ICI 204,448 is a potent κ-opioid agonist with potential analgesic activity for the study of neurological diseases.</p>

<p>NNC 63-0532 is a potentnociceptin receptor agonist, Ki=7.3 nM, EC50=305 nM.</p>

<p>CAY10786 (GPR52 antagonist-1) is an antagonist of G protein-coupled receptor 52 (GPR52, IC50 = 0.63 μM).</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>Faxeladol: adrenergic, serotonin inhibitor &amp; opioid agonist for neurological studies.</p>

<p>GPR40/FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1) agonist and allosteric modulator.</p>

<p>JNJ-20788560 is a delta opioid receptor (DOR) agonist with analgesic activity. It is more selective for DOR than for mu opioid receptors (MOR).</p>

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

<p>SCH-486757 is an agonist of nociceptin-1 (NOP1) and orphanin FQ peptide receptors and is used in the study of cough.</p>

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

<p>IPAG is a potent σ-receptor antagonist (pKi=4.3). IPAG can induce cell apoptosis.</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>Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-</p>

<p>GR 89696 fumarate is a highly selective κ2 opioid receptor agonist (IC50 = 0.04nM) with anti-pruritchy, anti-injury and neuroprotective effects.</p>

<p>ZD-6888 Hydrochloride, an angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension.</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>TC-MCH 7c is an oral, selectable and blood-brain barrier penetrating MCH1R antagonist with IC50 performance of 5.6 nM against hMCH1R, and TC-MCH 7c is a</p>

<p>Posatirelin, a synthetic peptide, modulates and nourishes brain systems, aiding in vascular dementia research.</p>

<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>Zindoxifene (D 16726) is an anti-estrogenic compound with antitumor activity that can be used in studies of breast and prostate cancer.</p>

<p>LY88074, a raloxifene analog sans basic side chain, is an ERβ agonist (EC50 = 232 nM) that promotes uterine cell growth.</p>

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

<p>Orotirelin (CG 3509), a TRH analog, counters pentobarbital sleep; may aid in cerebral ischemia.</p>

<p>Terlakiren (CP-80,794) is a renin inhibitor that inhibits the potency of human renin and can be used to study neurological disorders of the hypertensive type.</p>

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

<p>Apomine inhibits HMG-CoA-reductase, induces myeloma cell apoptosis, modulates myeloma, and boosts lovastatin's antitumor effects.</p>

<p>ONC1-13B, an androgen receptor antagonist, is used potentially for the treatment of prostate cancer.</p>

<p>Buloxibutid: a novel AT2 receptor agonist, Ki=0.4 nM (AT2), 10 μM (AT1).</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>Endoxifen HCl, a Tamoxifen metabolite, targets estrogen receptors more effectively and blocks aromatase, showing promise for breast cancer research.</p>

<p>Ralaniten triacetate (EPI-506) is a precursor of Ralaniten, an AR-NTD inhibitor, which can be used in the study of prostate and breast cancer.</p>

<p>BMS-641988 is a novel nonsteroidal androgen receptor antagonist for the treatment of prostate cancer.</p>

<p>Ripisartan (UP-269-6) is a potent and specific angiotensin II receptor antagonist that inhibits angiotensin II-mediated sympathetic tachycardia responses.</p>

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

<p>Palazestrant, an antiestrogen and antineoplastic agent, effectively targets ER+/HER2+ cancer when used in conjunction with a HER2 inhibitor.</p>

<p>SQ 32970 is a potent Endothia aspartic proteinase inhibitor.</p>

<p>PD 125754 is a Renin inhibitor, which represents a group of pharmaceutical drugs used primarily to treat essential hypertension.</p>

<p>Nur77 modulator 2: Kd of 0.35 μM, oral anti-inflammatory, affects Nur77/mitochondria localization.</p>

<p>PF 00277343, a thyroid receptor agonist, is used for the treatment of androgenetic alopecia.</p>

<p>ADL-08-0011 is an metabolite of alvimopan.</p>

<p>L 681176 is an inhibitor of the angiotensin-converting enzyme.</p>

<p>Frakefamide: potent analgesic, μ-selective agonist, non-CNS penetrating.</p>

<p>JNJ-17148066 is an agonist of estrogen receptor ESR1.</p>

<p>Compound 165: Potent estrogen receptor antagonist; useful for metastatic disease research.</p>

<p>Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].</p>

<p>Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (</p>

<p>CITFA, a GPER agonist, enhances neurite outgrowth in rat embryonic (E18) hippocampal neurons [1].</p>