g-protein

G-Protein antagonist peptide acetate is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide acetate inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis

Using specific antisera raised against synthetic peptides, we find that three distinct GTP-binding protein alpha subunits remain bound to the plasma membrane even after activation with nonhydrolyzable GTP analog. Trypsin cleaves each alpha subunit at a si

Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

mSIRK (G-Protein βγ Binding Peptide) is a cell-permeable activator of ERK 1 2 with an EC50 of 2.5-5 μM. It disrupts the interaction between the α and βγ subunits, facilitating α subunit dissociation without inducing nucleotide exchange [1].

G-418 disulfate (Geneticin sulfate) is an aminoglycoside antibiotic that selectively inhibits eukaryotic protein synthesis by blocking peptide chain elongation.

Obestatin (rat) acetate is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin (rat) acetate has anti-inflammatory, anti-myocardial infarction and antioxidant properties. Obestatin (rat) acetate suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain.

Neuropeptide FF acetate(99566-27-5 free base) (NPFF acetate) is an octapeptide belonging to the RF amide family. NPFF interacts with G-protein-coupled receptors NPFF (1) and NPFF (2).

BigLEN (mouse) acetate is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM.

Apelin-13 triTFA is the endogenous ligand of the APJ receptor, activating this G protein-coupled receptor with an EC50 value of 0.37 nM.

BAM (8-22) acetate is a proteolytically cleaved product of proenkephalin A. BAM (8-22) acetate activates Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner.

PKG Substrate acetate is a selective substrate for cGMP-dependent protein kinase (PKG).PKG Substrate is a selective substrate for protein kinase G (PKG) with a strong preference for PKG Iα (Km = 59 μM) over PKG II (Km = 305 μM).

[Lys8, Lys9]-Neurotensin (8-13) acetate, a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2, with Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively[1].

TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling.

TLQP 21 acetate is a potent agonist of G-protein-coupled receptor complement-3a receptor 1 (C3aR1). The EC50 values are 10.3 μM for mouse and 68.8 μM for human. TLQP 21 acetate is a VGF-derived peptide with endocrine and extraendocrine properties.

Protein Kinase C Peptide Substrate acetate targets specific cell spacers ina manner that is dependent on second messengers and specific adaptor proteins in response to extracellular signals that activate g protein-coupled receptors, tyrosine Kinase recept

Neuropeptide S (Rat) acetate is an endogenous ligand of a previously orphan G-protein-coupled receptor now named NPS receptor. Neuropeptide S (Rat) acetate can be used for the research of nervous system disease [1].

Endothelin-2 (49-69), human (Human endothelin-2), is a 21-amino-acid vasoactive peptide that binds to G-protein-coupled receptors ET-RA and ET-RB.

Alamandine TFA , a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine TFA targets to protect the kidney and heart through anti-hypertensive actions[1][2].

Vasopressin acetate, a cyclic nonapeptide, is synthesized centrally in the hypothalamus. Vasopressin acetate acts as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors.

ATI-2341 acetate is an effective allosteric agonist of CXCR4, it activates Gα1 instead of Gα13. ATI-2341 acetate activates inhibitory heterotrimeric G protein (GI) to promote the inhibition of cAMP production and induce calcium mobilization.

A 779 is a potent antagonist of the G-protein-coupled receptor Mas, the Ang1-7 receptor, which is distinct from conventional AngII.

Y16 acetate(429653-73-6 free base) is a G-protein–coupled Rho GEFs inhibitor; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

Tirzepatide acts as an agonist for both the glucagon-like peptide 1 receptor (GLP-1R) and G protein-coupled receptor 119 (GPR119), effectively inducing cAMP production in HEK293 cells that express either human GLP-1R or GPR119, with EC50 values of 6.54 and 1.01 nM, respectively. Additionally, at a concentration of 100 nM, it triggers receptor internalization in these cells. In vivo studies demonstrate that tirzepatide, administered at 10 nmol/kg per day, significantly reduces body weight, food intake, as well as plasma and hepatic triglyceride levels, free fatty acids (FFAs), leptin, and blood glucose in mice with high-fat diet-induced obesity. Furthermore, a dose of 50 nmol/kg every three days prevents an increase in eosinophils and lymphocytes in the bronchoalveolar lavage fluid (BALF) and inhibits bronchoconstriction prompted by methacholine in mice models of both asthma and diabetes, indicating its potential in treating type 2 diabetes mellitus.

Rhodopsin peptide is a peptide with the sequence H2N-Val-Ser-Lys-Thr-Glu-Thr-Ser-Gln-Val-Ala-Pro-Ala-OH, MW= 1217.33. Rhodopsin is a biological pigment in photoreceptor cells of the retina that is responsible for the first events in the perception of ligh

[Leu15]-Gastrin I human (Amino Acid Sequence Glp-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Leu-Asp-Phe-NH2) encodes for the protein [Leu15]-Gastrin I in human. In human chromosome, the gene GAST is localized on 17q21.2. G cells in the stomach antrum produces the precursor of [Leu15]-Gastrin I, progastrin.Progastrin undergoes cleavage and processing to yield gastrin, which is trophic for the entire gastrointestinal epithelium. Gastrin is essential for the growth of the digestive system and stimulates the production of gastric acid by parietal cells. Gastrin exerts its function through G-protein-coupled receptor called the cholecystokinin (CCK) or CCK-B receptor (CCK-BR). Gastrin release is stimulated by food, especially protein diet and is inhibited by very low pH. Atrophic gastritis, a Helicobacter pylori infection and long-term administration of proton pump inhibitors infection may cause overexpression of gastrin. Gastric adenocarcinoma show high levels of gastrin.

Endothelin-3, human, mouse, rabbit, rat TFA is a 21-amino acid vasoactive peptide that specifically interacts with G-protein-linked transmembrane receptors [ET-RA and ET-RB].

ATI-2341 is a potent, functionally selective allosteric agonist of the C-X-C chemokine receptor type 4 (CXCR4), acting as a biased ligand that prefers Gαi activation over Gα13. This compound activates the inhibitory heterotrimeric G protein (Gi), leading to reduced cAMP production and enhanced calcium mobilization. ATI-2341 effectively mobilizes bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) [1] [2].

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].

TRV055 hydrochloride, a Gq-biased ligand and G-protein-biased agonist of the angiotensin II receptor type 1 (AT1R), effectively stimulates cellular Gq-mediated signaling [1].

Proadrenomedullin N-terminal 12 peptide (PAMP-12), an endogenous fragment originating from the adrenal medulla and spanning amino acids 9-20 of human PAMP-20, plays a role in causing hypotension. It functions as an agonist for the MAS-related G protein-coupled receptor family member X2 (MRGPRX2), inhibiting forskolin-stimulated cAMP accumulation in CHO cells expressing human MRGPRX2 (EC50 = 57.2 nM) and selectively prompting calcium mobilization in these cells (EC50 = 41 nM), but not in cells expressing MRGPRX1, MRGPRX3, or MRGPRX4 at 1 µM. As an antagonist of nicotinic acetylcholine receptors (nAChRs), PAMP-12 obstructs carbachol-triggered catecholamine release and the influx of calcium and sodium (IC50s = 1.3, 0.39, and 0.87 µM, respectively) in primary bovine adrenal chromaffin cells, with no effect on histamine-induced responses (IC50s = >1 µM for all). Additionally, it decreases mean arterial blood pressure in normotensive rats at doses ranging from 10 to 50 nmol/kg.

Neuropeptide Y (NPY) is a 36-amino acid neuropeptide that exerts its activity via G-protein-coupled receptors. NPY is widely distributed in the peripheral and central nervous systems. It modulates a variety of physiological processes, e.g. the central reg

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

Vasomera, a stable, long-acting vasoactive intestinal peptide (VIP) agonist, targets G-protein-coupled VPAC2 receptors and is employed in the study of cardiomyopathy associated with dystrophinopathies [1].

Neuromedin S (human), a 33-amino acid neuropeptide, serves as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4 TGR-1, and acts on the neuromedin U (NMU) receptor 2 (NMUR2) to regulate body weight homeostasis [1].

Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)), is a nine-amino acid neuropeptide produced by the posterior pituitary gland. It plays a crucial role in maintaining fluid balance, osmolality, and cardiovascular function through interaction with three distinct G-protein coupled receptors (GPCRs): Avpr1a (V1a), Avpr1b (V1b), and Avpr2 (V2). Argipressin (diacetate) also influences centrally regulated metabolic processes, highlighting its significance in physiological regulation [1].

Apelin-36(rat, mouse) TFA, an endogenous agonist for the orphan G protein-coupled receptor APJ, exhibits a strong affinity for APJ receptors with an IC 50 of 5.4 nM and effectively inhibits cAMP production with an EC 50 of 0.52 nM. Moreover, it obstructs the invasion of certain HIV-1 and HIV-2 strains into NP-2/CD4 cells that express the APJ receptor [1] [2].

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells expressing the APJ receptor. [1] [2] [3] [4]

Apelin-17(human, bovine) TFA is an endogenous agonist of the orphan G protein-coupled receptor APJ, demonstrating affinity for human APJ receptors on HEK 293 cells with a pIC50 value of 9.02. It also blocks the entry of certain HIV-1 and HIV-2 strains into NP2 CD4 cells that express the APJ receptor [1] [2] [3].

Neuropeptide AF (cattle), an amidated octadecapeptide and RFamide neuropeptide, serves as a ligand for Mas-related gene receptor A4 (MrgprA4) (Mas-related G-protein-coupled Receptor (MRGPR)) with an EC50 of approximately 60 nM, and MrgprC11 with an EC50 of around 300 nM. It activates G protein-coupled receptors NPFF1 (Neuropeptide Y Receptor) with an EC50 ranging from ~25 to 325 nM, and NPFF2 with an EC50 of approximately 1 to 5 nM. Additionally, Neuropeptide AF (cattle) exhibits anti-opiate effects and modulates related pain [1] [2].

Apelin-13 is a 13-amino acid peptide sequence found in the central and peripheral nervous system that is an endogenous ligand for the G protein-coupled receptor angiotensin II protein J (APJ), with an EC50 value of 0.37 nM for APJ.Apelin-13 has vasodilatory and antihypertensive activity and can be used to study type 2 diabetic syndrome. Apelin-13 has vasodilatory and antihypertensive activities and can be used to study type 2 diabetes syndrome.

Apelin-13 is an endogenous ligand of APJ receptor, and the EC 50 value of activated G protein coupled receptor is 0.37 nM.

ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p

Obestatin (human) is an endogenous ligand for G-protein eurythmic entity 39 formed by shearing of preproghrelin, which inhibits feeding in a dose-dependent manner, and can be used in the study of obesity.

PKG Substrate is a selective substrate for cGMP-dependent protein kinase (PKG), showing a strong preference for PKG Iα (Km = 59 µM) over PKG II (Km = 305 µM).

Vasopressin Dimer (anti-parallel) TFA, an anti-parallel dimer form of vasopressin, has the capability to activate four G protein-coupled receptors: V1aR, V1bR, V2R, and OTR [1].

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biologically active peptide functioning as a selective agonist for Protease Activated Receptor 1 (PAR-1) [a subtype of G-protein coupled receptors involved in mediating thrombin's cellular effects]. Exhibiting high specificity for PAR-1 over PAR-2, its selectivity was assessed via cell-based calcium signaling assays in HEK293 cells. As an agonist, it is instrumental for in vivo investigations of PAR-1 activation. PAR-1 also collaborates with PAR-4, influencing thrombin-induced hepatocellular carcinoma within [coagulation type] tumor environments where thrombin generation occurs.

Neuromedin S(rat) TFA, a 34-amino acid peptide derivative of rat Neuromedin S, is a neuropeptide sourced from the rat brain that functions as a ligand for the G protein-coupled receptor FM4/TGR-1 [1].

Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and >100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent.