Endocrinology

Pantethine is an orally active lipid-lowering agent. Pantethine has anti-tumor, anti-inflammatory and anti-SARS-COV virus activities. Pantethine is also a neuroprotective agent. Pantethine can be used in the study of Alzheimer's disease, Parkinson's disease, major depression, systemic sclerosis and pantothenate kinase-related neurodegeneration.

Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.

Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.

Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K⁺ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects.

JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC₅₀ of 0.32 nM. JMS-17-2 impairs metastatic seeding and colonization of breast cancer cells.

Ceramides Mixture is an endogenous ceramide and consists of hydroxy and non-hydroxy fatty acid-containing ceramides. Ceramides Mixture is a main lipid component of the permeability barrier in epidermis. Ceramides Mixture is involved in the regulation of growth inhibition, cell cycle arrest, and modulation of telomerase activity.

Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation ^[1][2].

Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC₅₀ of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC₅₀ value of 200 nM.

Labetalol (AH5158) is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.

4-Methyl-2-oxopentanoic acid (α-Ketoisocaproic acid) is a metabolite of L-leucine and is involved in energy metabolism. 4-Methyl-2-oxopentanoic acid increases endoplasmic reticulum stress, promotes lipid accumulation in preadipocytes and insulin resistance by impairing mTOR and autophagy signaling pathways. 4-Methyl-2-oxopentanoic acid also causes oxidative damage, leading to cognitive deficits, inhibits α-ketoglutarate dehydrogenase activity, acts as an oxidative phosphorylation uncoupler and metabolic inhibitor. 4-Methyl-2-oxopentanoic acid acts as a nutrient signal and stimulates skeletal muscle protein synthesis. 4-Methyl-2-oxopentanoic acid can be used in the study of maple syrup urine disease.

Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC₅₀ values of 0.6±0.1 and 6.2±1.2 nM, respectively.

Melanotan I (MT-I; [Nle4,D-Phe7]-α-MSH) is an α-MSH (HY-P0252) analog, synthetic melanotropic peptide, and melanocortin receptor (MCR) agonist. Melanotan I induces skin tanning by mimicking the action of α-MSH on the melanocortin 1 receptor (MC1R) in melanocytes. As an appetite suppressant, Melanotan I impairs the ability of insulin to inhibit endogenous glucose production, suppresses leptin secretion from adipose tissue, and thereby reduces voluntary feed intake in ewes. Melanotan I can be used in research related to UV-induced skin damage, polymorphic light eruption, ruminant feeding, and sexual dysfunction.

Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC₅₀=1.8 and 1.7 nM, respectively; K_i=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC₅₀ values of 6, 44, 7, 4, 9, and 25 nM, respectively.

Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research.

Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion.

Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.