Endocrinology/Hormones

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

<p>Enalapril is a dicarbocyl-containing peptide and angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.</p>

<p>ER ligand-7 is a ligand for the estrogen receptor (ER) that can be used as a target protein ligand for synthesizing PROTAC ER Degrader-15.</p>

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

<p>Bufrolin is a potent GPR35 agonist, mast cell stabilizer, and anti-inflammatory research agent.</p>

<p>Ethamoxytriphetol is a non-steroidal estrogen antagonist.</p>

<p>Nurr1 agonist 9 (Compound 36) acts as an agonist for Nurr1, with an EC50 of 0.090 µM and a Kd of 0.17 µM. It activates Nurr1 homodimers (NurRE, EC50 = 0.094 µM) and Nurr1-RXR heterodimers (DR5, EC50 = 0.165 µM). This compound induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in Parkinson's disease organoid models and can penetrate the human brain endothelial cell barrier.</p>

<p>PSDalpha, a conjugate of PS, TB, and 17β-estradiol, degrades ERα with peak absorption at 465 nm, effectively inhibiting MCF-7 cell growth.</p>

<p>Arylpyrazole-based glucocorticoid agonist with potent anti-inflammatory effects; doesn't affect insulin secretion.</p>

<p>non-peptide δ1 opioid receptor agonist</p>

<p>Clocinnamox mesylate: irreversible μ-opioid blocker; Ki: 0.7 nM (mouse μ), 1.9 nM (δ), 5.7 nM (κ).</p>

<p>TD-802, an AR-targeting PROTAC with microsomal stability, shows promise for castration-resistant prostate cancer.</p>

<p>GNE-502 is an orally active and potent estrogen receptor (ER) degrader, specifically designed for research on breast cancer.</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>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>Galloylalbiflorin, an AR antagonist with IC50 53.3μM, is sourced from Paeonia lactiflora roots, exhibiting anti-androgenic properties.</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>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>CP 85339 is an aspartic acid protease inhibitor for X-ray analysis of peptide-renin complexes.</p>

<p>PD 125967 is a renin inhibitor, which represents a group of pharmaceutical drugs used primarily to treat essential hypertension.</p>

<p>[Met5]-Enkephalin, amide activates δ and ζ opioid receptors; has multiple forms and varying plasma levels.</p>

<p>Angiotensin II constricts blood vessels and boosts blood pressure by escalating norepinephrine release.</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>Epi-Cryptoacetalide is a useful organic compound for research related to life sciences and the catalog number is T126054.</p>

<p>Cgp 29287 is a primate-specific renin inhibitor. It also has a prolonged duration of action.</p>

<p>KOR agonist 4 (compound 39) is an agonist targeting the κ opioid receptor (Kappa Opioid Receptor) and activates G protein signaling. It has an EC50 of 14 nM and an Emax of 83% for binding to GTPγS. This compound demonstrates moderate to high intrinsic clearance in human liver cells and shows selectivity for the κ opioid receptor over the μ (MOR) and δ (DOR) opioid receptors by factors of 60 and 810, respectively. KOR agonist 4 is useful for research into central nervous system (CNS) disorders.</p>

<p>ARD-2585 is an orally active and selective androgen receptor PROTAC degrader with anticancer activity for the study of prostate cancer.</p>

<p>Methyl-2-quinolone from Evodia rutaecarpa blocks angiotensin II receptor with 48.2 μM IC50.</p>

<p>PD 132002 is a renin inhibitor.</p>

<p>Boc-ypgflt(O-tbu) is a delta-receptor-selective opioid antagonist.</p>

<p>Myrciacetin from Rhododendron inhibits rat aldose reductase with IC50 of 13 μM.</p>

<p>ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme(IC50s of 80 nM and 22 nM, respectively).</p>

<p>Competitive non-selective angiotensin II antagonist.</p>

<p>Nurr1 agonist 12 (Compound 37) acts as an agonist of the nuclear receptor-related protein 1 (Nurr1), enhancing its transcriptional activity with an EC50 of 0.06 μM. It stimulates human response elements NBRE, NurRE, and DR5 with EC50 values of 0.07 μM, 0.027 μM, and 0.014 μM, respectively. Additionally, Nurr1 agonist 12 induces the expression of neurotrophic genes regulated by Nurr1, such as tyrosine hydroxylase (TH), SOD1/2, BDNF, Sestrin 3, and BIRC5 (Survivin). The compound also demonstrates neuroprotective effects against neurotoxicity caused by Paraquat.</p>

<p>MT-7716 hydrochloride is a selective agonist of non-peptide nociceptin receptor (NOP)</p>

<p>"AZ'6421: A PROTAC degrading estrogen receptor alpha; potent in anti-tumor activity, useful for cancer research."</p>

<p>Potent GPR171 agonist (EC50 = 1.6 nM). ProSAAS-derived peptide. Regulates body weight in mice and promotes the outgrowth of neurites in Neuro2A cells.</p>

<p>ER degrader 5: potent ER degrader, anti-cancer, for breast cancer research.</p>

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

<p>BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC-type degrader (AR: DC50= 3.7 nM; AR-V7: DC50= 3.0 nM; GSPT1: DC50= 1.2 nM). It facilitates the ubiquitination and degradation of AR/AR-V7 and, through molecular glue properties, induces a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 is applicable in prostate cancer research.</p>

<p>RU-39411 is a steroidal anti-estrogen.</p>

<p>Enclomiphene-d4 is the deuterium-labeled analog of Enclomiphene. Enclomiphene functions as a potent and orally active estrogen receptor antagonist, exhibiting antiestrogenic properties.</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>LO-4-25 is a covalent degrader targeting the androgen receptor (AR) and its splice variant AR-V7. It covalently binds to the E3 ubiquitin ligase CUL4 DCAF16, facilitating the ubiquitination of both AR and AR-V7, which are then recognized and degraded by the proteasome, leading to reduced protein levels of AR and AR-V7 in cells. LO-4-25 is promising for research on androgen-independent prostate cancer.</p>

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

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

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

<p>Compound 5o, a Nurr1 agonist, exhibits neuroprotective properties as a transcription factor Nurr1 agonist, possessing a dissociation constant (Kd) of 0.5 μM and</p>

<p>ZINC05925939 is an estrogen receptor β (ESR2) inhibitor used in breast cancer research.</p>

<p>BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).</p>

<p>Antidiabetic agent 15 (compound 1B15) acts as a dual inhibitor of AT1R and NEP, reducing oxidative stress and restoring mitochondrial membrane potential.</p>

<p>(S,S)-J-113397 is an isomer of J-113397 . J-113397 is an Opioid Receptor antagonist [1] .</p>

<p>Frakefamide TFA: potent, peripherally active μ-opioid agonist; doesn't cross blood-brain barrier.</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>Inocoterone acetate is a nonsteroidal antiandrogen that binds to the androgen receptor and possesses antiandrogenic activity in animal models.</p>

<p>AM-5262 is a potent GPR40 Full Agonist with improved rat PK profile and general selectivity profile.</p>

<p>(Glu2)-TRH: Stable TRH analog; reduces TRH's cholinergic action; no thyroliberinase metabolism; neuroprotective with antidepressant, anticonvulsant effects.</p>

<p>ERα degrader12 (Compound RA3) is an estrogen receptor alpha (ERα) degrader with antitumor properties. It significantly suppresses tumor growth in a xenograft mouse model of breast cancer.</p>

<p>Rofleponide is a synthetic glucocorticosteroid with a high affinity for the rat thymus glucocorticoid receptor.</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>ER degrader 4, a selective and orally active compound, effectively degrades estrogen receptors and exhibits anti-tumor activity [1].</p>

<p>Orally active DPP-4 inhibitor/GPR119 agonist, Compound 22 lowers glucose, moderate hERG inhibition, IC50 4.9 µM, for diabetes research.</p>

<p>RLA-4842: iron-based anti-androgen; inhibits mCRPC cell proliferation.</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>Bexirestrant is an orally active ER-α degrader commonly employed in the research of antiestrogen and antineoplastic therapies.</p>

<p>GPR88 agonist 2 (compound 53) serves as a potent, brain-penetrant agonist of GPR88, exhibiting an EC50 of 14 µM in the GPR88 cAMP functional assay [1].</p>

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

<p>Bradykinin potentiator-5 is a peptide inflammatory mediator, causes blood vessels to dilate (enlarge), and therefore causes blood pressure to fall.</p>

<p>Opioid receptor agonist1 (Compound 2638-28) is an orally active opioid receptor agonist that shows strong affinity for MOR, DOR, and KOR, with Ki values of 5, 24, and 212 nM, respectively. It exhibits analgesic activity in both the mouse warm water tail-flick model and the acetic acid writhing model.</p>

<p>ER ligand-8 is a ligand of the estrogen receptor (Estrogen Receptor/ERR) and can be used for the synthesis of the PROTAC molecule ERD-1233.</p>

<p>ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor/ERR) ligand and a linker, utilized in the synthesis of PROTACs ERD-1233.</p>

<p>Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. It targets ERα for degradation through the ubiquitin-proteasome system by utilizing the E3 ubiquitin ligase component N-recognin 5. This compound is applicable in cancer research. (Pink: ERα inhibitor; Black: linker; Blue: CRBN Ligand)</p>

<p>THR-β Agonist 6, a selective and orally active compound targeting the thyroid hormone receptor β (THR-β), demonstrates specificity with EC50 values of 0.03 μM</p>

<p>CP-472555 is a selective nonsteroidal glucocorticoid receptor antagonist with anti-GR and anti-obesity activity in animal models.</p>

<p>N-terminally acetylated Endomorphin-1 is a modified Endomorphin-1.</p>

<p>Lactandrate is a homo-aza-steroidal ester of p-bis(2-chloroethyl) amino phenyl acetic acid.</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>Estrogen receptor modulator13 (Compound 5D) is an estrogen receptor antagonist with significant cytotoxic effects on MCF7 cells, exhibiting an IC50 value of 8.50 μM. Estrogen receptor modulator13 holds potential for breast cancer research.</p>

<p>PRL 2915 is a potent antagonist of the human somatostatin subtype 2 receptor (hsst 2), exhibiting a binding affinity (K_i) of 12 nM [1].</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>Gluten exorphin B5 (GE-B5) is a food-derived opioid peptide identified in digests of wheat gluten.</p>

<p>2-PCCA hydrochloride, a racemate, is a potent and selective GPR88 receptor agonist showing inhibition of GPR88-mediated cAMP production in HEK293 cells with an</p>

<p>OP-3633: potent GR antagonist (IC50: 29 nM), low PR agonism, AR antagonism, inhibits GR transcription.</p>

<p>Locicortolone is a synthetic glucocorticoid corticosteroid which was never marketed.</p>

<p>Linuron herbicide disrupts photosynthesis and acts as an androgen receptor antagonist.</p>

<p>N-Desmethyl Loperamide is the major metabolite of loperamide. It is also used as the precusor for radiolabelled loperamide.</p>

<p>3-MCPD ester found in edible oils, highest in olive pomace; toxic to mouse kidneys and spermatids.</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>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>Ludaterone is an antiandrogen agent, with potent antiandrogenic activity.</p>

<p>SR 43845 is an inhibitor of renin.</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>SRD5A1-IN-1 inhibits SRD5A1 with IC50 of 1.44µM, reducing dihydrotestosterone and SRD5A1 expression.</p>

<p>Calcitonin from eel regulates calcium and is key in studying postmenopausal osteoporosis.</p>

<p>PRO20 is a specific and competitive antagonist of the (pro)renin receptor (PRR). It inhibits the calcium influx induced by Proproin with an IC50 value of 81 nmol/L. By blocking the binding of Prorenin to PRR, PRO20 inhibits the activation of the renin-angiotensin system (RAS), reducing the production of angiotensin II (Ang II) and exerting antihypertensive effects. PRO20 holds promise for research in antihypertensive agents.</p>

<p>Antihypertensive agent 2 (Compound 4g) exhibits effective antagonistic activities against angiotensin II receptor 1 and reduces blood pressure with equal or</p>

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

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

<p>3-Cl-Pyridine-amide-acrylaldehyde-piperazine serves as a synthetic intermediate for LO-4-25. LO-4-25 is a ligand for the androgen receptor (AR) DNA binding domain and is linked to a truncated fumaramide handle via a connector. In 22Rv1 cells, LO-4-25 demonstrates potent degradation of both AR and AR-V7.</p>

<p>Tetrahydro Aldosterone is a steroidal compound that inhibits the adrenal angiotensin II receptor, with an IC50 of 10 μM.</p>

<p>Commendamide, natural, mimics N-acyl-amides, activates GPR132 with EC50 of 11.8 μM, made by Cbeg12 gene in commensal bacteria.</p>

<p>RG 13647 is an agonist of angiotensin II peptide.</p>

<p>Valorphin (Valorphin TFAsalt) has opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM.</p>

<p>Diisononyl phthalate (DINP), known as a plasticizer, is a phthalate. DINP is specifically a mixture of various isononyl esters of phthalic acid.</p>

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

<p>Prednisolone farnesylate is a novel transdermal corticosteroid with anti-inflammatory activity.</p>

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