Endocrinology/Hormones

<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>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>[Sar1,Ile8]-Angiotensin II (TFA) contracts arteries and affects cell growth in vascular muscle.</p>

Competitive non-selective angiotensin II antagonist.

<p>Faznolutamide is an antiandrogen agent [1] [2] .</p>

<p>Nociceptin peptide fragment (1-11) with potent ORL1/KOR-3 receptor agonism (Ki = 55 nM), no opioid receptor affinity, and analgesic in mice.</p>

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

<p>4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetrical cyclic non-steroidal estrogen. It exhibits high binding affinity to estrogen receptors ERα and ERβ.</p>

<p>TLB 150 Benzoate (RAD150) is a modulator of the androgen receptor with an IC50 value of 0.13 μM.</p>

<p>Methylpiperidino pyrazole is an ERα inhibitor and can prevent the BPS-induced Rb phosphorylation and cell cycle progression.</p>

<p>AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.</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>RLA-4842: iron-based anti-androgen; inhibits mCRPC cell proliferation.</p>

<p>Emd 55068 is a synthetic antagonist of renin.</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>TRV055 acetate is a ligand of angiotensin II type 1 receptor and stimulates cellular Gq-mediated signaling.</p>

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

<p>ARD-266 is a PROTAC degrader based on the von Hippel-Lindau E3 ligase that induces the degradation of AR proteins and is useful in prostate cancer research.</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>Strong, selective NOP receptor antagonist with pKi=10.24; &gt;3000x selectivity over δ, μ, κ receptors; blocks nociceptin effects.</p>

<p>Latanoprost acid is a prostanoid receptor agonist that blocks RANKL and can be used to reduce intraocular pressure.</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>Norethindrone acetate (19-Norethindroneacetate) is an oestrogen with inhibitory effects on adolescent menstruation and hepatic adenomas and is often used in</p>

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

<p>Gridegalutamide exhibits anti-androgen and anti-tumor activities.</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>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>(S)-CVN424 modulates GPR6, key for neurological/psychiatric research, including Parkinson's.</p>

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

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

<p>ST-CY14 is an inhibitor of the Nur77-PPARγ interaction with an EC50 of 3.15 μM. It binds to Nur77 (Kd=32 nM) to prevent its ubiquitination and degradation by PPARγ, reducing fatty acid uptake and mitochondrial respiration, and inhibiting the transcription of CD36 and FABP4. ST-CY14 suppresses proliferation and migration of MCF7 and MDA-MB-231 cancer cells and impedes tumor growth and bone metastasis in mouse models.</p>

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

<p>ER modulator 6 (3a) is a potent ERβ agonist with a K i of 0.44 nM; 19x more selective for ERβ than ERα.</p>

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

<p>AKR1B10-IN-1: potent AKR1B10 inhibitor, IC50 3.5 nM; hinders lung cancer cell growth, spread, and Cisplatin resistance.</p>

<p>Yp537 acts as an estrogen receptor (ER) inhibitor, specifically preventing the dimerization of the human estrogen receptor [1].</p>

<p>Dipropyl phthalate is a weak androgen receptor inhibitor, and can be used in biochemical experiments and drug synthesis.</p>

<p>Potent, oral AR-V7 degrader (Compound 6); DC50: 0.32µM; targets AR-DBD via VHL E3; EC50: 0.88µM in 22Rv1 cells.</p>

<p>4A7C-301, a Nurr1 agonist, exhibits potent neuroprotective effects in vitro and markedly mitigates neuropathological abnormalities while enhancing motor and</p>

<p>Ro 64-6198: Nonpeptide, selective NOP agonist, high brain uptake, EC50=25.6 nM, 100x NOP&gt;opioid affinity.</p>

<p>[Orn8]-Urotensin II is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.</p>

<p>ARCC-4: A VHL-recruiting, low-nanomolar (DC50=5nM) AR degrader; outshines enzalutamide; degrades AR mutants resistant to therapy.</p>

<p>Parathyroid hormone (PTH) receptor agonist. Increases serum PTH levels and bone mass in rats.</p>

<p>Biphalin TFA is an opioid peptide analog that penetrates the blood-brain barrier (BBB) and encompasses two active enkephalin pharmacophores.</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>Betamethasone acibutate, a glucocorticoid, is derived from Betamethasone.</p>

<p>Remikiren is a highly specific renin inhibitor with oral activity for the treatment of hypertensio.</p>

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

<p>2-Ethylhexyl trans-4-methoxycinnamate is a sunscreen agent.</p>

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

<p>Aliskiren (CGP 60536) D6 Hydrochloride is a deuterium-labeled Aliskiren. Aliskiren hemifumarate is a direct and orally active renin inhibitor (IC50: 1.5 nM).</p>

<p>Angiotensin amide, an octapeptide amide, can be used to increase blood pressure by vasoconstriction.</p>

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

<p>T4-ATA S-isomer, the active form of the thyroid hormone, represents the S-isomer of T4-ATA.</p>

<p>It is a metabolite of tamoxifen and an estrogen receptor modulator.</p>

<p>1α-Hydroxy-3-epi-vitamin D3, a natural metabolite derived from 1alpha,25-dihydroxyvitamin D3, effectively suppresses parathyroid hormone (PTH) secretion[1].</p>

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

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

<p>Herkinorin: μ-opioid agonist with 100x μ-affinity, 50x less κ-affinity than Salvinorin A, from Salvia divinorum. Semi-synthetic from Salvinorin B.</p>

<p>NOP site high affinity ligand (Ki=1.5 nM); blocks nociceptin effects in rat brain/heart; agonist in vivo, reduces mouse movement.</p>

<p>ALR2-IN-6 (compound 9) is a potent competitive inhibitor of ALR2, with a Ki value of 0.064 μM. It is applicable in research related to neuropathy, retinopathy, and nephropathy.</p>

<p>Ac-RYYRWK-NH2: potent, specific NOP receptor partial agonist with 0.071 nM affinity; no affinity for μ/κ/δ-opioid receptors.</p>

<p>Antitumor agent-195 (compound 16c) is a dual-targeting agent that simultaneously targets STAT3 and NQO1. At a concentration of 1 μM, it significantly inhibits the phosphorylation of STAT3 at the Tyr705 site and effectively induces apoptosis in MDA-MB-231 and MDA-MB-468 breast cancer cells. As a substrate of NQO1, Antitumor agent-195 markedly increases ROS production, causing severe DNA damage in a dose-dependent manner. It also demonstrates strong antitumor properties in MDA-MB-231 xenograft models.</p>

<p>THR-β agonist 2 diacetate (Compound 3) is a potent THR-β agonist with potential applications in researching metabolic disorders such as obesity, hyperlipidemia, hypercholesterolemia, and diabetes, as well as other conditions like steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis, and other related diseases and conditions.</p>

<p>PTP1B/AKR1B1-IN-2 (Compound 7f) is a potent inhibitor targeting both PTP1B and AKR1B1 with IC50 values of 3.2 and 2.1 μM, respectively, and K i values of 4.0</p>

<p>'[Sar1, Ile8]-Angiotensin II acetate triggers oxidases and prompts superoxide in muscles; has varied vascular impacts.</p>

<p>L 363564 is a kidney renin inhibitor.</p>

<p>MCH (salmon) TFA is a 19-amino-acid neuropeptide affecting appetite, energy, sleep, and heart health via GPCR SLC-1/GPR24 and MCHR2.</p>

<p>GPR171 agonist from ProSAAS controls mouse appetite, reduces glutamate in paraventricular neurons via G protein.</p>

<p>(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1, which is an estrogen-related receptor alpha (ERRa) degrader.</p>

<p>PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group.</p>

<p>PROTAC ER Degrader-4 is a PROATC degrader of estrogen receptor (ER)(IC50 of 0.8 nM).</p>

<p>Floramanoside C exhibits 2,2-diphenyl-1-picrylhydrazyl scavenging and aldose reductase inhibitory activities [1].</p>

<p>Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain</p>

<p>HINT1-IN-1 (compound 8) is an inhibitor of histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. It influences the cross-regulation between μ-opioid receptors (MOR) and NMDA receptors (NMDAR).</p>

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

<p>OT-R antagonist 2 is a nonpeptide low molecular weight antagonist of OT-R .</p>

<p>BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.</p>

<p>3-epi-25-hydroxy Vitamin D3 lowers serum PTH in male weanling rats at 0.5 and 1 IU/g doses; doesn't affect females.</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>Alunacedase alfa (APN-01) is an angiotensin-converting enzyme 2 with antiviral activity.</p>

<p>Perindoprilat (Perindoprilate) is an angiotensin-converting enzyme inhibitor.</p>

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

<p>CGP 38560 is a potent renin inhibitor.</p>

<p>Nurr1 agonist 2 with EC50 of 0.07 μM, boosts TH &amp; VMAT2 mRNA, binds Nurr1 LBD at Kd 0.14 μM, for parkinsonism study.</p>

<p>Dynorphin (1-8) is an opioid octapeptide from the porcine hypothalamus. It comprises the N-terminal eight residues of dynorphin.</p>

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

<p>Selective NOP receptor partial agonist peptide; Ki=0.71 nM; &gt;4000 nM for μ, δ, κ receptors; boosts food intake in vivo.</p>

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

<p>Azilsartan Medoxomil Potassium (TAK-491 Potassium) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.</p>

<p>Zavacorilant is capable of modulating glucocorticoid receptor (GR).</p>

<p>FFA2 modulator; inhibits cAMP, enhances 35SGTPγS binding (pEC50: 6.9, 7.23); alters Gi/Gq signaling; affects lipolysis, neutrophil migration.</p>

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

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

<p>NH-3, an orally active THR antagonist with a 55 nM IC50, blocks thyroid hormone binding and cofactor recruitment.</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>Antihypertensive agent 2 (Compound 4g) exhibits effective antagonistic activities against angiotensin II receptor 1 and reduces blood pressure with equal or</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>PF-06478939 TFA is a peptide that acts as a non-brain-penetrating agonist at the oxytocin (OT) and vasopressin receptors, exhibiting EC50 values of 0.01 nM and</p>