Endocrinology/Hormones

<p>PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein.</p>

<p>Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derived from Estrone that specifically binds to estrogen receptor α (ERα).</p>

<p>Deacylcortivazol is a potent glucocorticoid that inhibits growth in glucocorticoid-resistant leukemia cells without receptor mediation.</p>

<p>μ opioid receptor agonist; IC50: 5.5 nM (μ), &gt;10,000 nM (δ). Induces reversible analgesia, catalepsy, hyperthermia in rats.</p>

<p>TRV056 is a Gq-biased AT1R agonist effective in Gq-mediated signaling and a basis for similar drug development.</p>

<p>DP32 is a dual-function compound incorporating an opioid receptor (MOP) agonist and a neuropeptide FF receptor (NPFFR) antagonist. It is applicable in analgesia-related research.</p>

<p>Awl 60 is a substance P (6-11) non-competitive antagonist.</p>

<p>(S)-CVN424 modulates GPR6, key for neurological/psychiatric research, including Parkinson's.</p>

<p>RTI-13951-33 HCl: potent, selective GPR88 agonist; brain-penetrant; EC50 = 25nM; curbs rat alcohol behaviors.</p>

<p>Retosiban is an effective and selective oxytocin antagonist (Ki: 0.65 nM).</p>

<p>TF-505, a steroid 5α-reductase inhibitor, is used potentially for the treatment of benign prostatic hyperplasia.</p>

<p>Angiotensin IV analog, potent HGF/c-MET inhibitor (IC50=3 pM), halts MDCK cell growth and invasion, AT4 antagonist, impairs LTP, antiangiogenic.</p>

<p>VinclozolinM2-2204 is an androgen receptor AUTOTAC degrader with a DC50 of 200 nM in LNCaP prostate cancer cells. It induces the formation of AR+LC3+ autophagic membranes and is applicable for cancer research.</p>

<p>DP50 is a bifunctional compound containing both an opioid receptor agonist (MOP) and a neuropeptide FF receptor (NPFFR) antagonist. It can be utilized in studies related to analgesia.</p>

<p>Olmesartan impurity, related to parent RNH-6270, is an AT1R antagonist used for hypertension research.</p>

<p>Cgp 44099 is a potent plasma renin inhibitor from all subprimate species.</p>

<p>17-Epiestriol, metabolite of estrone, forms via 16α-hydroxy intermediate and binds ERα and ERβ with affinity less than 17β-estradiol.</p>

<p>Potent, selective OP4 agonist; pKi=10.68, pEC50=9.80. &gt;8000x selectivity vs other opioid receptors; long-lasting in vivo effects.</p>

<p>ERα degrader10 is a potent, selective, orally active estrogen receptor α (ERα) degrader. It demonstrates strong ERα binding affinity (IC50 of 24.0 nM) and degradation capability (EC50 of 5.3 nM). This compound degrades ERα through a proteasome-mediated pathway and is utilized in breast cancer research.</p>

<p>Emd 55068 is a synthetic antagonist of renin.</p>

<p>Nocistatin, a neuropeptide, blocks Nociceptin effects and inhibits 5-HT release, acting on an opioid-related receptor.</p>

<p>PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist that activates the G protein signaling pathway with an EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). Additionally, PIPE-3297 promotes myelination and has anti-inflammatory properties.</p>

<p>PD 123177 is an inhibitor of Nonpeptide angiotensin AII-2.</p>

<p>Rac-Finerenone, or (Rac)-BAY 94-8862, is an oral nonsteroidal MR antagonist with high selectivity and an IC50 of 18 nM.</p>

<p>AKR1Cs-IN-1 (Compound 29) is an effective and broad-spectrum inhibitor of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). It achieves subtype inhibition by simultaneously binding to the SP2 and SP3 pockets, thereby blocking metabolic pathways related to drug resistance. In enzyme assays, AKR1Cs-IN-1 exhibits significant inhibitory activity with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM for AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. The compound shows excellent resensitizing effects in doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, effectively enhancing the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on breast cancer resistance.</p>

<p>A unique collection of xnum potassium channel blockers and agonists for high throughput and high content screening;</p>

<p>Akuammicine, as an indole alkaloid from Catharanthus roseus, can be used in cancer cell eradication.</p>

<p>A unique collection of xnum compounds targeting histaminergic receptor and melatonin receptor for high throughput screening (HTS) and high content screening (HCS</p>

<p>GRA-1, an arylpyrazole, is a potent glucocorticoid receptor agonist with robust anti-inflammatory effects and preserves insulin secretion.</p>

<p>Montirelin is an analog of thyrotropin-releasing hormone.</p>

<p>'[DAla2, DArg6] Dynorphin A (1-13) porcine is a potent opioid peptide resistant to enzymatic degradation.'</p>

<p>AKR1C3-IN-10 (compound 5r), a selective inhibitor of AKR1C3 with an IC50 of 51 nM, demonstrates efficacy in a prostate cancer xenograft model [1].</p>

<p>UT receptor ligand acts mainly as silent antagonist with slight agonist effects; blocks U-II in rat aorta, pIC50 = 7.46, &amp; inhibits plasma leakage in mice.</p>

<p>RLA-5331: iron activator with anti-androgen properties; inhibits mCRPC cell proliferation.</p>

<p>Rat Brain Natriuretic Peptide (1-32) is a 32-amino-acid peptide from heart, released when ventricles stretch excessively.</p>

<p>Dermorphin Analog, a heptapeptide from amphibian skin, binds μ-opioid receptors selectively and strongly.</p>

<p>Compound 114 (D3R/MOR antagonist 1) exhibits dual antagonistic activity at dopamine D3 receptors (D3R) and mu-opioid receptors (MOR), with K i values of 46.5 nM</p>

<p>Imidaprilate, an active TA-6366 metabolite, is a potent ACE inhibitor with an IC50 of 2.6 nM, researched for hypertension.</p>

<p>[Sar1, Ile8]-Angiotensin II(3TFA) is a peptide that has multiple effects on vascular smooth muscle.</p>

<p>OT-R antagonist 1: Nonpeptide, selective, low-weight blocker of oxytocin; IC50 = 8 nM for Ca2+ disruption.</p>

<p>ERD-308, potent at 5nM, achieves &gt;95% ER degradation in ER+ breast cancer, with DC50 of 0.17-0.43 nM.</p>

<p>Urotensin-II receptor antagonist, no agonist effect, pEC50 7.24, blocks U-II in rat aorta assay.</p>

<p>Ocedurenone, a corticosteroid receptor antagonist, is a compound utilized in the investigation of kidney disease (WO2018054357, compound I).</p>

<p>TAN67 is the first effective selective non-peptide delta1 opioid receptor.</p>

<p>PAC, based on WO2017201449A1's LP2, enhances ERα degradation; used in making ADCs with PROTAC-linker, it's attached to antibodies.</p>

<p>PF-0251802 HCl is a bio-active chemical.</p>

<p>Hydrocortisone sodium succinate is a glucocorticoid which is used to alleviate allergic reactions, particularly those of the skin and gums.</p>

<p>Human Urotensin II (114-124) is an 11-amino acid peptide with vasoconstrictor properties and agonizes GPR14.</p>

<p>SNIPER(ER)-110 links cIAP1 and estrogen ligands. SNIPER(ER)-51 degrades ER protein; DC50 &lt;3 nM at 4h, 7.7 nM at 48h.</p>

<p>CNP, from natriuretic family, first in pigs, now in other species, processes into CNP-22/CNP-53, similar to ANP/BNP, with varying potencies.</p>