Endocrinologie/Hormones

Competitive non-selective angiotensin II antagonist.

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

Orphine is an opioid compound that can amplify the antinociceptive effects reduced by naloxone in mice.

Ludaterone is an antiandrogen agent, with potent antiandrogenic activity.

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

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.

Triamcinolone benetonide is a synthetic glucocorticoid corticosteroid exhibiting potent anti-inflammatory properties.

Parathyroid Hormone (1-34), bovine is a PTH receptor agonist used to study osteoporosis and hypoparathyroidism.

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

Ripafollitropin alfa (bovine) is a fusion protein that combines recombinant follicle-stimulating hormone with chorionic gonadotropin [1].

Biotin-Oxytocin (Biotin-α-Hypophamine; Biotin-Oxytocic hormone) is a biologically active peptide. It is oxytocin labeled with biotin at the N-terminus.

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

Urotensin II, mouse TFA is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

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

RG 13647 is an agonist of angiotensin II peptide.

Naldemedine (S 297995), developed by Shionogi, is a drug for opioid side effects like constipation. It's well tolerated with minor GI issues.

AKR1C3-IN-9: Selective AKR1C3 inhibitor, IC50=8.92 nM; reverses DOX resistance in breast cancer.

MT-7716: selective NOP agonist, potential in preventing alcohol abuse/relapse.

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

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

3-MCPD ester found in edible oils, highest in olive pomace; toxic to mouse kidneys and spermatids.

<p>EX-A5386 (Glucocorticoid receptor modulator-1) is a potent glucocorticoid receptor modulator, IC50/EC50&lt;100nM.</p>

ER degrader 5: potent ER degrader, anti-cancer, for breast cancer research.

Compound PDK0283, with CAS No. 58-72-0, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound PDK0283 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

Angiotensin II is a potent direct vasoconstrictor, causing arteries and veins to constrict, so leading to an increase in blood pressure.

Nesvacumab (REGN910) is a fully human monoclonal antibody targeting Angiopoietin 2 (Ang2), which can be used for studying advanced solid tumors.

N-terminally acetylated Endomorphin-1 is a modified Endomorphin-1.

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

[Asp5]-Oxytocin acetate: a biologically active neurohypophyseal hormone analogue, inducing uterine contractions, effects magnified by Mg2+.

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

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

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

OT antagonist 1 demethyl derivative is the demethyl derivative of OT antagonist 1. OT antagonist 1 is a selective Oxytocin antagonist (Ki of 50 nM. )

(Val3,Pro8)-Oxytocin functions primarily as a Gq-dependent pathway agonist and exhibits secondary activity as a reduced efficacy agonist for β-arrestin

BPRMU191 is a distinct mu-opioid receptor (MOR) modulator with an EC50 of 2.17 μM in FLIPR Ca2+ assays conducted on CHO-K1/MOR/Gα15 cells. Additionally, BPRMU191 interacts with MOR in the presence of naloxone.

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

CSD-CH2(1,8)-NH2 is a selective and competitive kappa-opioid receptor (KOR) antagonist with a K i of 6.8 nM.

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

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

N-Acetyl-α-Endorphin is a chemical compound consisting of α-Endorphin that has been acetylated at the N-terminal.

DALDA TFA is a potent, μ-opioid receptor agonist exhibiting high selectivity and an affinity constant (K i) of 1.69 nM.

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

Rofleponide is a synthetic glucocorticosteroid with a high affinity for the rat thymus glucocorticoid receptor.

AH 8529 is an orally active opioid compound with analgesic properties.

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.

Oxytocin analog with glycine at position 9; impacts health, development, reproduction, behavior.

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

PD 123177 is an inhibitor of Nonpeptide angiotensin AII-2.

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.

Renin FRET Substrate I, designed for human renin, contains angiotensinogen's N-terminal cleavage site.

Deltorphin (Dermenkephalin) is Isolated from the skin of Phyllomedusa Sauvage. It also has an affinity to the opioid receptor.

Selective δ opioid antagonist. Exhibits partial agonist in vitro activity at δ receptors at high concentrations.

N-Phenethylnoroxymorphone is an opioid compound that can enhance morphine-induced analgesia in rats. It is used in the research of neurological disorders.

KOR agonist 3 (Compound 5) is an agonist of the κ opioid receptor (κOR) with an EC50 of 0.88 nM. It also exhibits some activation of μOR, with an EC50 of 720 nM. However, KOR agonist 3 does not activate δOR at concentrations below 1 μM. Its ability to recruit β-Arrestin-2 is lower than that of U50488.

Pro8-Oxytocin, a modified oxytocin (OXT) ligand, elicits more potent and efficacious responses at primate OXTR and induces stronger behavioral effects compared

Saprisartan (GR-138950, GR-138950X) is an AT1 receptor antagonist used for the treatment of heart failure and blood pressure.

Hemorphin-7, an atypical opioid peptide from hemoglobin, may enhance memory, promote cell growth, and is a potential breast cancer biomarker.

SNC 80, a non-peptide δ-opioid agonist (Ki=1.78 nM, IC50=2.73 nM), also targets μ-δ heteromers (EC50=52.8 nM), with analgesic and antidepressant potential.

BAY 1003803 is a glucocorticoid receptor agonist for the topical treatment of psoriasis or severe atopic dermatitis.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader.

Corynantheidine ((-)-Corynantheidine) is a partial agonist of the mu opioid receptor (MOR) and demonstrates MOR-dependent analgesic effects in mice.

Displays functional MCH-antagonist and MSH-agonist activity in different behavioral paradigms.

6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone), a water-soluble ester, is used for allergic, cardiac, and hypoxic emergencies.

<p>Norethindrone acetate (19-Norethindroneacetate) is an oestrogen with inhibitory effects on adolescent menstruation and hepatic adenomas and is often used in</p>

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

Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the

<p>Dexamethasone phosphate is a synthetic adrenal corticosteroid. It also has potent anti-inflammatory properties.</p>

"ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH)

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

ET Receptor Antagonist 1 (compound 16h), with an IC50 value of 0.18 nM, is an orally active agent that can be utilized for pulmonary arterial hypertension (PAH

<p>Anticancer agent 135 (compound 26h) acts as a potent androgen receptor (AR) antagonist, effectively blocking AR nuclear translocation and inhibiting AR/AR-V7</p>

Androgen Receptor Antagonist 9 (compound 28) serves as an antagonist to the androgen receptor [1].

<p>WCA-814, an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate, induces degradation of both full-length and AR-V7, exhibiting cytotoxic effects in</p>

Vasopressin Dimer (parallel) TFA, a parallel dimer of Vasopressin, has the capability to activate four G protein-coupled receptors—namely, V1aR, V1bR, V2R, and

<p>Dynorphin A (1-10) is an opioid peptide, binds κ-opioid receptor, blocks NMDA current, IC50: 42.0 μM.</p>

Compound 181, also known as 14-3-3σ/ERα Stabilizer-1, is a covalent stabilizer targeting the 14-3-3σ/ERα proteins.

AH 7959 is an orally active N-substituted cyclohexylmethylbenzamide compound that exhibits analgesic properties. In mice, the ED50 for oral and subcutaneous administration of AH 7959 exceeds 100 mg/kg.

ERD-3111 (Compound 44), an orally active PROTAC ERα degrader (DC50: 0.5 nM), exhibits efficacy in inhibiting tumor growth in both the parental MCF-7 xenograft

2-sec-Butylphenol is an inhibitor of the androgen receptor and P450 aromatase, and can be used in research and experiments in the field of life sciences.

ngiotensin II 5-valine is an angiotensin II analog which is an agonist at angiotensin receptors.

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH)

ERα degrader 6 (Compound 31q) is an ERα degrader with a K I of 75 nM and also inhibits ARO with an IC50 value of 37.7 nM.

Dynorphin B (1-9), a neuropeptide and the N-terminal cleavage product of dynorphin B, has its formation inhibited by N-ethylmaleimide (NEM), a non-selective

CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

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

AP-238 is a novel synthetic opioid (NSO) that acts as an agonist for the μ-opioid receptor (MOR), with an EC50 of 248 nM. Additionally, AP-238 exhibits analgesic properties.

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.

ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a K d value of 6.5 μM.

R4K1 is a cell-permeable stapled peptide that binds with high affinity to estrogen receptor (ER) α, inhibiting its interaction with coactivators. It penetrates breast cancer cells, regulating gene transcription and suppressing cell proliferation. R4K1 is applicable for tumor research.

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

Emd 55068 is a synthetic antagonist of renin.

Keap1-IN-1 (Compound 27) is an inhibitor of Keap1, functioning by covalently modifying the Cys151 residue on the BTB domain of KEAP1, thereby disrupting the interaction between Keap and Nrf. It enhances the mRNA expression of the antioxidant response element (ARE) dependent gene NQO1, with an EC50 of 160 nM, and exhibits cytotoxicity in U2OS cells, with an EC50 of 527 nM.

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

LY2623091, a mineralocorticoid receptor antagonist, is utilized in treating refractory hypertension. It demonstrates CYP3A4-dependent clearance and exhibits synergistic effects when combined with CYP3A4 inhibitors.

Zankiren is a renin inhibitor. Zankiren can reduce blood pressure, plasma renin activity, and angiotension II.

11-Ketodihydrotestosterone is a metabolite of 11β-Hydroxyandrostenedione. It is an active androgen and is also a potent androgen receptor (AR) agonist (Ki: 20.4 nM, EC50: 1.35 nM for human AR).

ERα/ERβ antagonist-1 (Compound 10) functions as a partial antagonist of both ERα and ERβ. It reduces the activity of ERα and ERβ in HepG2 liver cells in a dose-dependent manner.

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

Koreanoside E is a useful organic compound for research related to life sciences. The catalog number is T125538 and the CAS number is 1804014-67-2.