GPCR/G-Protein

ONO-8711 is a potent and selective competitive antagonist of EP1 receptor with Kis of 0.6 nM and 1.7 nM for human and mouse EP1, respectively.

[D-Pro4,D-Trp7,9,10] Substance P (4-11) serves as a potent antagonist of the tachykinin family of neuropeptides [1].

N-Methyl-2-phenylpropan-1-amine hydrochloride is an analogue of β-methylphenethylamine (BMPEA) and demonstrates neurotransmitter-releasing properties in experiments involving NET and DAT.

GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. Corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.

Brain Natriuretic Peptide-45, rat TFA (BNP-45, rat TFA) is an isoform of rat brain natriuretic peptide extracted from rat heart, exhibiting significant

Neuropeptide Y (29-64), amide, human is a biologically active 36-amino acid peptide.

Alosetron, a 5-HT3 antagonist, is used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in women only.

CYM 5442 HCl: potent, selective S1P1 agonist (EC50 = 1.35 nM), induces MAPK activation & lymphopenia, brain-penetrant.

L-797,591 is a selective agonist of somatostatin receptor subtype 1.

2-Furoyl-LIGRLO-amide TFA is a peptide that acts as a proteinase-activated receptor-2 (PAR2) agonist, and contains a furoyl group addition at its N-terminal.

<p>AC-263093 is an NPFFR2 agonist with anxiolytic activity that increases c-Fos protein expression in the paraventricular nucleus of the hypothalamus.</p>

4-Methylamphetamine hydrochloride is a 5-HT1A receptor agonist that induces a decrease in body temperature in rats by binding to the 5-HT1A receptor. Additionally, it increases the extracellular levels of neurotransmitters norepinephrine (NE), dopamine (DA), and serotonin (5-HT) by affecting their transporters. 4-Methylamphetamine hydrochloride is applicable in the study of neurological disorders.

Guanylin (mouse, rat) TFA is a peptide composed of 15 amino acids and acts as an activator of intestinal guanylate cyclase. This compound is utilized in research related to diarrhea.

Satavaptan is a vasopressin V2 receptor antagonist. Satavaptan improves the control of ascites in cirrhosis.

15(S)-15-methyl Prostaglandin F2α methyl ester can be used in related research in the field of life sciences.

ent-8-iso Prostaglandin F2α is a potent vasoconstrictor of porcine retinal and cerebral microvessels with EC50 values of 30.6 and 53.5 nM, respectively.

Compound 11: potent antipsychotic, binds 5-HT1A/2A/2C, D2, H1 receptors; K is 56.6-1140 nM, BBB permeable.

<p>FLLRN is a biologically active peptide serving as a PAR1-specific antagonist.</p>

ANP (1-30), frog, a peptide fragment sourced from atrial natriuretic peptide of frog origin, exhibits natriuretic, diuretic, and vasorelaxant properties.

LCKLSL, an N-terminal hexapeptide, inhibits AnxA2 and tPA binding, reduces plasmin, and exhibits anti-angiogenic effects.

<p>Potent, orally active APJ receptor agonist 4; EC50: 0.06 nM, Ki: 0.07 nM; good pharmacokinetics in rodent HF model; safe in studies; boosts cardiac function.</p>

Liraglutide acetate is the acetate salt form of Liraglutide, which is a glucagon-like peptide-1 (GLP-1) receptor agonist, utilized in the study of type 2 diabetes.

Pegapamodutide (LY-2944876) is a dual glucagon-GLP-1 receptor agonist utilized in research concerning type 2 diabetes and obesity [1].

Dabelotine, (S)- is the S-isomer of Dabelotine. Dabelotine is an adrenergic agonist used in the study of dementia.

<p>A unique collection of xnum compounds targeting histaminergic receptor and melatonin receptor for high throughput screening (HTS) and high content screening (HCS</p>

GPR183 antagonist-3 (compound 33) is an orally active GPR183 antagonist with an IC50 value of 8.7 μM. It demonstrates significant in vitro anti-migration and anti-inflammatory activity in monocytes and can alleviate pathological symptoms in experimental colitis induced by dextran sulfate sodium.

Flunarizine is an orally administered peripheral vasodilator, a dual blocker of voltage-gated Na+/Ca2+ channels and a D2 dopamine receptor antagonist.

H 409-22 isomer formic, a formate salt of Y1 receptor antagonist 1, is an antagonist of the neuropeptide Y1 receptor (neuropeptide Y1 receptor). This compound effectively blocks the actions of the receptor, playing a crucial role in modulating physiological responses.

PACAP (6-38) is a PACAP receptor blocker with IC50s of 30, 600, 40 nM for type I, VIP1, and VIP2 receptors.

Amylin (IAPP), feline is the peptide subunit of amyloid found in pancreatic islets of type 2 diabetic patients and in insulinomas.

<p>Bradykinin (1-3) is a fragment of Bradykinin. Bradykinin is an activates pain receptors.</p>

AB21 HCl: σ1 receptor antagonist, Ki 13 nM; less potent at σ2 (102 nM). Reduces mechanical hypersensitivity.

20-SOLA is the first water-soluble 20-HETE antagonist with oral bioavailability. It significantly improves blood pressure changes and kidney damage associated with the streptozotocin (STZ) diabetic mouse model. Additionally, 20-SOLA acts as a GPR75 receptor blocker. This compound is useful in research related to cardiovascular pathology.

GPR183, a chemotactic receptor aiding B cell maturation, binds 7α,25-OHC; studied in IBD research.

Palmitoyl tetrapeptide-20 (PTP20) TFA is a biomimetic peptide and acts as an agonist of α-MSH. It protects follicular melanocytes by boosting catalase expression and activating melanogenesis.

Ilatreotide is a Amadori compound of octreotide.

ANQ-11125 TFA is a motilin antagonist with a pKd of 8.24, inhibiting motilide contractions in rabbits.

<p>[Des-Arg10]-HOE I40 TFA is a potent antagonist of the bradykinin B1 receptor.</p>

GLP-1R Agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).

K-(D-1-Nal)-FwLL-NH2 TFA: potent ghrelin inverse agonist; Ki=4.9 nM (COS7), 31 nM (HEK293T); blocks Gq/G13 signaling.

Potent BB1, BB2, and BB3 agonist; IC50: 0.26, 1.55, 2.52 nM. Boosts glucose transport in myocytes, promotes cancer cell growth in vitro.

Conessine hydrobromide is a naturally occurring steroid alkaloid and has been used in traditional herbal medicine as a treatment for amoebic dysentery.

GB-6, a short linear peptide that selectively binds to the gastrin releasing peptide receptor (GRPR), shows potential as a high-contrast imaging probe due to

d[Leu4,Lys8]-VP acetate: Vasopressin V1b agonist. Ki: rat 0.16 nM, human 0.52 nM, mouse 1.38 nM. Low antidiuretic/vasopressor effects.

Phoenixin-14 TFA (PNX-14 TFA) is an endogenous neuropeptide that can modulate GnRH receptor expression and exerts anxiolytic effects.

A-286501: Oral adenosine kinase inhibitor, IC50=0.47 nM, reduces pain via non-opioid, non-NSAID ADO receptors.

Thioperamide maleate (MR-12842 maleate) is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31

Amylin, a 37-amino acid human hormone, moderates glucose regulation by reducing glucagon, delaying digestion, and increasing satiety.

Endogenous high affinity agonist for human NPY Y4 receptor (Ki = 0.056 nM). Believed to play an important role in the function of the gastrointestinal tract.

<p>cAC 253 acetate (TP2135 Free base) is an amylin antagonist. cAC 253 acetate inhibits 125I-adrenomedullin binding, with an IC50 of 25 nM.</p>

NK2 tachykinin receptor selective antagonist.

Peptide inhibits G protein-receptor binding; competitively blocks M2 and β-adrenoceptor-induced Gs/Gi/Go activation.

GUB03385 is a long-acting PrRP31 analogue and an effective dual agonist for GPR10 (full agonist, EC50: 0.4 nM) and NPFF2R (partial agonist, EC50: 20 nM), with anti-obesity properties.

Potent P2Y6 agonist

MRS 2957 triethylammonium salt is a P2Y6 agonist.

Cyclo(L-Leu-L-Trp) is a diketopiperazine metabolite initially derived from Penicillium, exhibiting antibacterial (MICs = 125-1000 µg/ml) and antifungal activities (MICs = 8-64 µg/ml). It also demonstrates antioxidant properties by reducing the production of hydroxy radicals, as evidenced in an electron spin resonance (ESR) spectroscopy assay (IC50 = 1.8 µM). Additionally, Cyclo(L-Leu-L-Trp) has been identified as a bitter compound capable of quickly crossing rat taste cell membranes ex vivo at a 1 mM concentration. Furthermore, it acts as a melatonin receptor agonist in X. laevis melanophores, suppressing cAMP accumulation at a 20 µM concentration, with this effect being negated by the melatonin receptor antagonist luzindole.

Eledoisin (Eledone peptide) is a specific agonist of NK2 and NK3 receptors.Eledoisin is an undecapeptide of mollusk origin, belonging to the tachykinin family

(Phe2,Orn8)-Oxytocin acetate: V1 agonist with EC50 of 280 nM for rabbit epididymis contractility.

DOTA-JR11 is a somatostatin receptor 2 (SSTR2) antagonist that can be radiolabeled with 68Ga.

ACTH (1-14) (TFA) is a regulatory fragment of adrenocorticotropin, specifically involved in the control of cortisol and androgen synthesis [1].

<p>CRF2 receptor antagonist; Kd 1.4 nM (mCRF2β), 153.6 nM (rCRF1). Blocks sauvagine-induced cAMP in cells &amp; stress-related responses in mice.</p>

Rhazimine is an indole alkaloid. It is a dual inhibitor of arachidonic acid metabolism and platelet activating factor-induced platelet aggregation.

15(R)-PTA2 is an (R)-epimer of PTA2; doesn't inhibit platelet aggregation or gastric tone; less effective than PTA2 at blocking prostaglandin contraction.

Pancreatic polypeptide TFA acts as a neuropeptide Y (NPY) Y4/Y5 receptor agonist.

<p>Losulazine: a new antihypertensive, requires functional sympathetic nervous system; mechanism undefined.</p>

Gamma-Glu-AbuTFA is the TFA salt form of Gamma-Glu-Abu. This compound acts as an agonist for the calcium sensing receptor (CaSR), activating CaSR in HEK-293 cells with an EC50 of 0.21 μM.

Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist with non-selective antagonism at recombinant and human platelet P2X1 receptors.

XAC dihydrochloride is an Adenosine A1 and A2 receptor antagonist with IC50s of 1.8 nM and 114 nM, also a mouse convulsant.

Glucagon receptor antagonist -1 is a highly effective glucagon receptor antagonist.

Atriopeptin III (rat) (ANP 127-150), a 24-amino acid atrial peptide, functions as a powerful vasodilator and natriuretic/diuretic agent, enhancing renal

Neurokinin A(4-10)(TFA) is an agonist of tachykinin NK2 receptor .

IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM).

BMY-14802 (alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol) is a selective and orally active sigma-1 antagonist with an IC50 of 112 nM.

1a,1b-dihomo Prostaglandin E1 is a class of prostaglandin compounds.

<p>PY-60 can effectively activate YAP transcriptional activity against annexin A2 (ANXA2).Cost-effective and quality-assured.</p>

Secretin (28-54), human TFA is a 27-amino acid peptide that works on the human Secretin receptor.

β-CGRP, human ,a 37-amino acid peptide,is the beta form of Calcitonin-gene-related peptide (β-CGRP), involved extensively in regulation of the cardiovascular

GLP-1(7-36), amide acetate is a derivative of GLP-1 peptide , activate the GLP-1 receptor, promote insulin secretion,Type 2 diabetes mellitus and obesity.

Maridebart is a humanized IgG1-kappa monoclonal antibody that targets the GIPR (gastric inhibitory polypeptide receptor) [1].

[18F]-Labeled L-dopa precursor is a precursor for synthesis of 18F-labeled L-dopa[1].

Bradykinin (1-7), an amino-truncated peptide derived from Bradykinin, is a metabolite formed through enzymatic cleavage by endopeptidase.

Guanylin (human) TFA, a 15-amino acid peptide, activates intestinal guanylate cyclase, regulating electrolyte and water transport via cGMP.

<p>(R)-Citalopram oxalate is a weak selective serotonin reuptake inhibitor (SSRI) that antagonises its S-isomer (escitalopram), anticonvulsant and antidepressant</p>

<p>Tryptamine hydrochloride is a monoamine alkaloid, metabolite of tryptophan and CNS active substance, agonist of 5-HT4 receptor, TAAR1, AHR.</p>

MRS-1706: Ki of 1.39nM for A2B; selective inverse agonist; also affects A2A, A1, A3.

S1PR1 modulator 1 is a selective inhibitor of S1PR1 with a pIC50 of 7.6.

Lu AA33810 is a selective neuropeptide Y5 (NPY5) receptor antagonist with an oral activity and BBB permeability, anti-anxiety and antidepressant-like effects.

Orexin B, rat/mouse TFA, activates OX1-R & OX2-R receptors, influencing food intake, energy, and sleep regulation.

(Phe2,Orn8)-Oxytocin: Selective V1 agonist, induces rabbit epididymis contractility, EC50=280 nM.

(+)-Chloprostol is a PGF2α agonist, mimics prostaglandin F2α, induces luteal dissolution in mares without side effects or stress.

Litoxetine HCl, an SSRI and 5-HT antagonist, treats urinary incontinence and relaxes rat oesophageal muscles without antimuscarinic effects.

G-Protein antagonist peptide acetate is a truncated substance P-related peptide, competes with receptor for G protein binding.

(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14), a bombesin (BBN) antagonist, holds potential for cancer research applications [1].

NF157, a selective P2Y11 antagonist with pKi 7.35, lowers MMP-3/MMP-13, aiding OA treatment; IC50s: P2Y11 463 nM, P2Y1 1811 μM, P2Y2 170 μM.

Urocortin III, a human peptide, binds CRF-R2, affecting insulin via somatostatin feedback with K i values 13.5-100+ nM.

Selective MC4 agonist with IC50: 0.58 nM (MC4), 55 nM (MC3); revives heart/lung function in shocked rats.

<p>FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar binding potency.</p>