Endocrinology/Hormones

<p>4',2-Dihydroxy-4,6-dimethoxydihydrochalcone, an estrogen-like compound, binds to bovine estrogen receptors, IC50 15 μM.</p>

<p>ngiotensin II 5-valine is an angiotensin II analog which is an agonist at angiotensin receptors.</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>Bovine adrenal medulla docosapeptide (BAM-22P) is a potent opioid agonist, derived from the proenkephalin A gene, which is present in the adrenal medulla.</p>

<p>Bioactive metabolite of nociceptin, antagonist of nociceptin-induced hyperalgesia</p>

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

<p>NPFF1-R antagonist 1 (compound 8b) is a piperidine analog and an effective neuropeptide FF (NPFF) receptor antagonist. It exhibits 15-fold selectivity for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.</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>OT-R antagonist 2 is a nonpeptide low molecular weight antagonist of OT-R .</p>

<p>Vasopressin Dimer (anti-parallel) TFA, an anti-parallel dimer form of vasopressin, has the capability to activate four G protein-coupled receptors: V1aR, V1bR,</p>

<p>Neuropeptide AF (human) acetate (Neuropeptide AF (human) acetate (192387-38-5 Free base)) is an anti-opioid neuropeptide, a Neuropeptide AF (human) derivative,</p>

<p>DAMGO is a selective peptide agonist of the µ-opioid receptor .</p>

<p>β-Endorphin, equine TFA, an endogenous opioid peptide, demonstrates high affinity binding to μ/δ opioid receptors and possesses analgesic properties [1] [2] [3</p>

<p>Frakefamide TFA: potent, peripherally active μ-opioid agonist; doesn't cross blood-brain barrier.</p>

<p>Cebranopadol hemicitrate is a NOP and opioid receptor agonist that targets human NOP, MOP, KOP, and δ-opioid peptide (DOP) receptors, with Ki/EC50 values of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, and 18 nM/110 nM, respectively. It is used in studies of acute and chronic pain.</p>

<p>Potent μ-receptor antagonist, Ki=0.96nM, ineffective at δ (&gt;10,000nM). Alters behavior in vivo, boosts K+ currents in rat neurons in vitro, μ-independent.</p>

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

<p>Methylprednisolone Acetate(Depo-Medrate) has the ability to inhibit oxygen free radicals and can be used to treat acute spinal cord injuries.</p>

<p>GNE-274, akin to GDC-0927 but non-degrading, is a partial ER agonist in breast cancer, enhancing chromatin at ER sites, inhibiting ER-LBD.</p>

<p>Teriparatide is an agonist of PHT(IC50 of 2 nM in HEK293 cells).</p>

<p>15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is a natural product that can be used as a reference standard. The CAS number of 15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is 420781-85-7.</p>

<p>Compound 121, a D3R/MOR antagonist with K i values of 361 nM and 85.2 nM for D3R and MOR respectively, has the potential for analgesic effects through MOR</p>

<p>β-Naltrexamine dihydrochloride is an orally administered, irreversible opioid receptor antagonist. Its derivatives exhibit optimised subtype selectivity and can be used for pain research.</p>

<p>7α-(Thiomethyl)spironolactone is a steroid receptor antagonist and major spironolactone metabolite, steroid metabolism, nuclear receptor, and coronavirus.</p>

<p>SL910102 is a nonpeptide angiotensin antagonist of the AT1 receptor.</p>

<p>7β-Hydroxy-epi-androsterone (7β-Hydroxy-EpiA) is an endogenous androgenic derivative of dehydroepiandrosterone that possesses the ability to bind to ERβ,</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>PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor/ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.</p>

<p>Potent μ opioid antagonist, IC50 3.5 nM, 1200x selectivity over δ and somatostatin, brain-penetrant, active in vivo.</p>

<p>Selective δ opioid antagonist. Exhibits partial agonist in vitro activity at δ receptors at high concentrations.</p>

<p>Osteostatin, derived from parathyroid hormone-related protein (PTHrP) 107-111, has demonstrated properties conducive to bone repair in animal models presenting</p>

<p>BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.</p>

<p>Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8.</p>

<p>Axelopran (TD-1211) treats opioid constipation; it's a potent, selective peripheral opioid blocker.</p>

<p>Hemorphin-7, an atypical opioid peptide from hemoglobin, may enhance memory, promote cell growth, and is a potential breast cancer biomarker.</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>ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a K d value of 6.5 μM.</p>

<p>β-Lipotropin (60-65) (β-LPH (60-65)), an opioid agonist, is a significant [1] opioid peptide.</p>

<p>Gridegalutamide exhibits anti-androgen and anti-tumor activities.</p>

<p>A 779 is a potent antagonist of the G-protein-coupled receptor Mas, the Ang1-7 receptor, which is distinct from conventional AngII.</p>

<p>PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), exhibiting inhibitory potency with IC50s</p>

<p>Displays functional MCH-antagonist and MSH-agonist activity in different behavioral paradigms.</p>

Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.

<p>Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor .</p>

<p>β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities.</p>

<p>WAY267464: nonpeptide OT agonist, anxiolytic, modulates selectivity, improves CNS entry and oral uptake.</p>

<p>Antihypertensive agent 3 (compound 4a), an angiotensin II receptor 1 antagonist, demonstrates antihypertensive activity in spontaneously hypertensive rats (SHRs</p>

<p>Alclometasone is a glucocorticoid that reduces inflammation and treats various skin conditions like eczema and psoriasis.</p>

<p>PROTAC AR Degrader-4: IAP ligand, linker, AR binder; it's a SNIPER that degrades AR non-genetically.</p>

<p>PROTAC ER Degrader-3 from patent WO2017201449A1 is a PAC synthesis intermediate for ADC/PROTAC antibody conjugates, boosting ERα degradation.</p>