Endocrinology/Hormones

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.

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

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

Emd 55068 is a synthetic antagonist of renin.

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

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

Helianorphin-19: Potent KOR agonist (Ki=25 nM; EC50=45 nM), 200x selective over μ/δ receptors, effective in mouse pain model, non-sedative.

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

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

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.

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

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

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

KYLO-0603 is an orally active and selective THR-β agonist with an EC50 of 31.07 nM. It effectively reduces serum cholesterol and low-density lipoprotein cholesterol levels. By activating THR-β receptors, KYLO-0603 enhances the expression of THR-regulated genes like iodothyronine deiodinase 1 (Dio1), malic enzyme 1 (Me1), and thyroid hormone-responsive (Thrsp) gene, while it inhibits the expression of inflammatory and fibrosis-related genes, including low-density lipoprotein receptor (LDL-R) gene. This compound is applicable for the study of metabolic associated steatohepatitis (MASH) and liver fibrosis.

E-2078, known chemically as (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8), is a stable analog of Dynorphin A (1–8) and functions as a kappa opioid

PRL 3195: Somatostatin antagonist, Ki: 6 nM (sst5), 17 nM (sst2), 66 nM (sst3), 1 μM (sst1/4).

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.

Prepro-TRH-(160-169), a pro-TRH peptide, enhances TRH-stimulated TSH secretion.

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.

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