nonpeptide

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.

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.

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.

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

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.

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.

BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.

Allisartan Isoproxil is a nonpeptide antagonist of angiotensin II receptor and can be used in studies about hypertension and heart diseases.

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.

PF3274167 (Cligosiban) is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.

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.

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.

Erlosiban, also known as OBE001, is a novel, orally active nonpeptide oxytocin receptor antagonist under development for the treatment of preterm labor and improvement in embryo implantation and pregnancy rate in assisted reproductive technology (ART).

BIBS-222, a nonpeptide angiotensin II (Ang II) receptor antagonist, appears to be an effective antihypertensive in the model of the renal hypertensive rat.

SM19712 sodium is an inhibitor of nonpeptide endothelin converting enzyme.

NBI-31772 hydrate is a powerful inhibitor of the interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). It acts as a nonpeptide ligand, effectively releasing bioactive IGF-I from the IGF-I/IGFBP-3 complex (Ki values for all six human subtypes range from 1-24 nM). This compound demonstrates significant anxiolytic and antidepressant-like effects [1] [2] [3].

ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35.

TW-37 is an nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 (Ki: 0.29 1.11 0.26 μM).

NVP-SAA164 is a nonpeptide bradykinin B1 receptor antagonist agent.

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

L-159282 is an orally active and nonpeptide angiotensin II receptor antagonist. It also has anti-hypertensive activity.

Fasitibant is a potent and selective nonpeptide kinin B2 receptor antagonist.

MK-0429 is an orally active, selective, and nonpeptide antagonist of αvβ3 integrin (IC50: 80 nM).

Cam 2445 is a nonpeptide, alpha-methyltryptophan derivative; an NK1 neurokinin receptor antagonist that is a potentially useful treatment for arthritis, asthma, migraine, anxiety, psychosis, and emesis.

Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients

Eprosartan (SKF-108566J free base) is a selective, competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes, used as an antihypertensive agent. It exhibits inhibitory effects on angiotensin II receptors with IC50 values of 9.2 nM in rat adrenocortical membranes and 3.9 nM in human adrenocortical membranes.

L-365260 is an orally available, selective and potent nonpeptide gastrin and cerebral cholecystokinin receptor (CCK-B) antagonist.L-365260 inhibits CCK-8S-induced increase in [Ca2+]i, blocks stress-induced hypersensitivity in viscera, and blocks the anti-exploratory effect of CCK-4.L-365260 has been used in the study of neurological Ojibwa and endocrine diseases.

YM 218 is a novel, potent, selective antagonist of nonpeptide vasopressin V1A receptor.

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).

AVE 0991, a nonpeptide analog of angiotensin-(1-7) [Ang-(1-7)], is an orally active Mas agonist with inhibitory effects on [125I]-Ang-(1-7) binding to bovine aortic endothelial cell membranes, and inhibits astrocyte-mediated neuroinflammation in Alzheimer's disease by enhancing autophagy.

PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1 FPR2 FPR3.

Avatrombopag hydrochloride (AKR-501) is an orally active, nonpeptide agonist of the thrombopoietin (TPO) receptor with an EC50 of 3.3 nM. It effectively mimics TPO by stimulating platelet production through activation of the intracellular signaling system, facilitating platelet and megakaryocyte generation from hemopoietic precursor cells. Additionally, Avatrombopag hydrochloride serves as a substrate for cytochrome P450 [CYP] 2C9 and CYP3A.

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.

L-159884 is a radiolabelled, nonpeptide angiotensin II antagonist that is useful for angiotensin II, AT1 receptor imaging

BIBS 39 is a novel nonpeptide angiotensin II (AII) receptor antagonist.

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.

Ici D8731 is a nonpeptide angiotensin II antagonist with potential as a treatment for hypertension and heart failure.

FR167344 free base is an orally active, nonpeptide antagonist of the bradykinin receptor B2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor.

YNT-185 is a nonpeptide, selective agonist of the orexin type-2 receptor (OX2R), with EC50 values of 0.028 μM for OX2R and 2.75 μM for OX1R. Additionally, YNT-185 effectively alleviates symptoms of narcolepsy-cataplexy in mouse models.

Fradafiban (BIBU-52) hydrochloride is a nonpeptide antagonist of the platelet glycoprotein IIb IIIa complex, exhibiting a dissociation constant (Kd) of 148 nM for binding affinity to the human platelet GP IIb IIIa.

PD 117302 is a nonpeptide opioid compound. It is a selective kappa-opioid agonist. PD 117302 causes naloxone-reversible locomotor impairment and diuresis. It is an Anti-Arrhythmia Agent, an Anticonvulsants, a Cardiovascular Agent, and a Central Nervous Sy

Lamifiban trifluoroacetate is an antagonist of the nonpeptide platelet fibrinogen receptor (GPIIb/IIIa).

Lamifiban is a nonpeptide glycoprotein IIb/IIIa antagonist. It prevents platelet loss during experimental cardiopulmonary bypass.

SR 146131 is a potent and selective agonist of the nonpeptide receptor.

WAY267464 is a nonpeptide small-molecule OT agonists with anxiolytic activity. WAY267464 may be used for modulation of potency, selectivity over the structurally similar vasopressin receptors, CNS penetration, and oral bioavailability.

SM19712 free acid is an inhibitor of nonpeptide endothelin converting enzyme.

MDL-105212A HCl is a nonpeptide NK-1 and NK-2 receptor antagonist.

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.