non-peptide

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.

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.

Proteinase K (Protease K) is a non-specific serine protease that can tolerate changes in SDS, urea, pH (4-12), salt concentration, and temperature. Proteinase K hydrolyzes a wide range of peptide bonds and is used for protein digestion.

Paliroden is a non-peptide compound that can be taken orally and is used for supplementing neuro-nutrition. It stimulates the synthesis of endogenous neurotrophic factors and is employed in the research of neurodegenerative diseases such as Alzheimer's and Parkinson's.

Lanepitant 2HCl is a non-peptide neurokinin-1 receptor antagonist with analgesic and anti-inflammatory activity.Lanepitant 2HCl inhibits the binding of Substance P to the neurokinin-1 receptor, inhibits neurogenic inflammation and pain transmission, and can be used in the study of painful neuropathic disorders, such as migraines.

Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

(R)-CJ 11974: non-peptide NK1 receptor antagonist, may relieve pain and prevent chemo-induced vomiting.

Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

Tirofiban(MK383) hydrochloride monohydrate is a non-peptide glycoprotein IIb/IIIa antagonist.

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

L-Norvaline is an arginase inhibitor and a non-protein branched-chain amino acid. L-Norvaline has previously been reported as a natural component of the antifungal peptide of Bacillus subtilis. L-Norvaline and other modified branched-chain amino acids have received attention in recent studies because they appear to be incorporated into some recombinant proteins found in E. coli.

H-Abu-OH (L-α-amino-n-Butyric acid) , also known as (S)-2-aminobutanoic acid, homoalanine, 2-AABA, ethylglycine, or L-butyrine, is a member of the class of compounds known as L-alpha-amino acids. H-Abu-OH is a non-proteogenic amino acid that can be found in the human kidney, in liver tissues, and in most biofluids or excreta (e.g. feces, breast milk, urine, and blood). Within the cell, H-Abu-OH is primarily located in the cytoplasm. H-Abu-OH is biosynthesized by transaminating oxobutyrate, a metabolite in isoleucine biosynthesis. As a non-proteogenic amino acid, H-Abu-OH can be used by nonribosomal peptide synthases.

Ibutamoren Mesylate (MK-0677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.

Argireline (Acetyl hexapeptide-3) is a peptide composed of amino acid chains that significantly inhibits Ca2+-dependent neurotransmitter (acetylcholine) release at the neuromuscular junction, exhibiting notable anti-wrinkle and anti-aging activity[1][2][3].

PF-184563 is an effective and selective non-peptide antagonist of the V1a receptor with oral activity, suitable for studying Raynaud's disease and dysmenorrhoea.

Anatibant is a potent non-peptide bradykinin B2 receptor antagonist. Anatibant reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury.

Galantide acetate, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide acetate recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide acetate dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide acetate appears to bind to a single population of SP receptors (KD~40 nM).

BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist.