nonpeptide

Ivachtin (Caspase-3 Inhibitor VII) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor(IC50 = 23 nM) and is a modest inhibitor of the remaining caspases.

SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.

Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition.

Lanepitant (LY303870) is a nonpeptide neurokinin-1 (NK-1) antagonist with analgesic activity that inhibits neurogenic dura mater inflammation and is used for the prevention of migraine.

L-162,313 is an ANG II receptor agonist, a nonpeptide that mimics the biological actions of angiotensin II and induces an increase in MAP.

Nebentan potassium (YM598) is an orally active and selective nonpeptide endothelin receptor (ETA receptor) antagonist.Nebentan potassium inhibits pulmonary arterial hypertension and may be useful in the study of neurologic and cardiovascular diseases.

AM-8123 is an orally available nonpeptide APJ agonist.AM-8123 reduces collagen load and improves cardiac function. AM-8123 ameliorates myocardial infarction in rats and can be used to study cardiovascular diseases such as heart failure.

SB273005 is an orally active and potent nonpeptide integrin αvβ3 antagonist that inhibits αvβ3 and αvβ5 and reduces the production of Th2 cells and the cytokine IL-10 in pregnant mice.

Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity.

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active small-molecule, nonpeptide thrombopoietin receptor agonist that stimulates megakaryopoiesis. It binds to and activates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), promoting the proliferation and differentiation of megakaryocytic cells and enhancing platelet production.

(R)-Elagolix (NBI-56418) is a short-acting, nonpeptide, GnRH antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively. administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses.

L-368,899 hydrochloride is an orally available and selective nonpeptide oxytocin receptor (OXTR) antagonist for the prevention of preterm labor.L-368,899 hydrochloride prevents oxytocin-induced anti-anomalous pain and anti-nausea, and may be useful for the study of depression.

LIT-001 free base improves social interaction in a mouse model of autism. LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM).

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

LMD-009 is a non-peptide, selective CCR8 agonist that mediates chemotaxis, inositol phosphate accumulation, and calcium release, with an EC50 of 11–87 nM.

OT-R antagonist 2 is a nonpeptide, low molecular weight antagonist of OT-R (oxytocin receptor).

OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

Proglumide hemicalcium is a antagonist of nonpeptide and orally active cholecystokinin (CCK)-A B receptors, has antiepileptic and antioxidant activities.

A-192621 is a potent, nonpeptide, orally active, and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and elevates both arterial blood pressure and plasma ET-1 levels[1][2][3]. Its selectivity is 636-fold higher for ETB than ETA (IC50 of 4280 nM and Ki of 5600 nM).

AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes, with IC50 of 21±35 nM. AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist.

Devazepide is a competitive and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor (IC50s: 81 pM, 45 pM, and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively).