activating

PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate) is an agonist of Protease-Activated Receptor-2 (PAR-2).

Proteasome-activating peptide 1 TFA is a potent activator of the proteasome, enhancing chymotrypsin-like proteasomal catalytic activity and thereby increasing proteolytic rates both in vitro and in culture. Additionally, it inhibits protein aggregation in cellular models of amyotrophic lateral sclerosis (ALS) [1].

Proteasome-activating peptide 1 enhances chymotrypsin-like proteasomal catalytic activity, boosting proteolytic rates both in vitro and within cultured cells. Additionally, it inhibits protein aggregation in a cellular model of amyotrophic lateral sclerosis [1].

Sperm-activating peptide 1 is a bioactive chemical.

SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is a protease-activated receptor-2 (PAR-2) agonist that induces non-histaminergic pruritus.

PACAP (1-38), human, ovine, rat (Pituitary Adenylate Cyclase Activating Polypeptide 38) is a neuropeptide with 38 amino acid residues.

PACAP (1-38), a novel neuropeptide isolated from the bovine hypothalamus is more active than vasoactive intestinal peptide (VIP) in stimulating adenylate cyclase (EC50=7 nM). PACAP 1-38 (10-9 M) increased substance P (SP), gastrin releasing peptide (GRP),

PACAP (6-27) (human, ovine, rat) serves as an antagonist for the PACAP receptor, inhibiting the catecholamine response of the canine adrenal gland to vasoactive intestinal peptide (VIP). This compound holds promise for research into cardiovascular and neurological disorders [1].

Hemorphin-7 acetate is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).

Octapeptide-2 Acetate, as a hair growth promotion active, is a double-layered encapsulated biomimetic peptide that helps increase cell growth and migration. It promotes hair growth by activating the stem cells of the hair follicles. Octapeptide-2 is more stable and prolongs action than native proteins.

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.

Cyclo(his-pro) is an endogenous cyclic dipeptide that exerts oxidative damage protection by selectively activating the transcription factor Nrf2 signalling pathway.

PACAP 1-38 acetate is a pituitary adenylate cyclase activating polypeptide (PACAP) analogue. PACAP 1-38 acetate binds to PACAP type I receptor(IC50 = 4 nM) and PACAP type II VIP2 receptor(IC50 = 1 nM) but not to PACAP type II, VIP1 receptor.

Uroguanylin-15 (Rat) is a bioactive natriuretic peptide hormone that modulates sodium excretion in response to high NaCl intake by activating guanylate cyclase signaling pathways in the intestine and kidney. Initially isolated from rat urine and duodenum, it shares functional similarities with guanylin but has not been detected in rat colon extracts.

[Glu1]-Fibrinopeptide B, a derivative of fibrinopeptide B amino acid residues 1-14, originates from human fibrinopeptide B (hFpB). hFpB is a proteolytic cleavage product of the fibrinogen B beta-chain, specifically generated by thrombin, which plays a significant role in activating neutrophils (PMN), monocytes, and fibroblasts.

Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml). Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).

MitTx-beta, a peptide isolated from the venom of the Texas coral snake (Micrurus tener tener), forms a complex with MitTx-α to comprise MitTx, which exhibits ASIC1 channel activating activity on capsaicin-sensitive nerve fibers [1].

Glucagon (22-29) acts as a partial agonist of Glucagon (19–29) and independently inhibits the calcium (Ca2+) pump in liver plasma membranes without activating adenylate cyclase [1] [2].

Mastoparan X, a tetradecapeptide derived from wasp venom, functions as a GTP-binding regulatory protein (G protein)-activating peptide. It directly activates G proteins coupled to phospholipase C, inducing secretion in various cell types [1].

[Lys8, Lys9]-Neurotensin (8-13) (JMV438) is a Neurotensin analog that elicits analgesic effects by activating the G protein-coupled receptors NTS1 and NTS2. The compound has K i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.

Ser-Ala-alloresact, a sperm activating peptide (SAP), plays a pivotal role in the fertilization process through its release from the eggs of marine invertebrates, facilitating sperm activation [1] [2].

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

Certepetide (CEND-1), also known as iRGD, is a bifunctional cyclic peptide that enhances tumor penetration. By interacting with alphav-integrins through its RGD motif and activating NRP-1, it transforms the solid tumor microenvironment into a temporary conduit for therapeutic agents. This property facilitates Certepetide's accumulation in tumors, making it a valuable tool in researching pancreatic cancer and other solid tumors [1] [2] [3].

LHC165, a toll-like receptor 7 (TLR7) agonist, stimulates the immune system's response by activating TLR7.

KRAS G13D peptide, a 25-mer sequence, is derived from the KRAS activating oncogene mutation and serves as an immune potentiator. This peptide possesses immunogenic properties and can be utilized for the development of a KRAS vaccine.

TAT peptide (TFA), a cell-penetrating peptide (GRKKRRQRRRPQ) originating from HIV-1's trans-activating transcriptional activator (Tat), facilitates intracellular delivery [1] [2].

Adipokinetic hormone II (Locusta migratoria) (Lom-AKH-II), an insect adipokinetic hormone (AKH), elevates fat body cAMP levels in vitro. These hormones (AKHs) regulate the mobilization of carbohydrates and lipids from fat body reserves for flight, by activating AKH receptor(s) that stimulate cAMP production and glycogen phosphorylase through the stimulatory guanine nucleotide-binding protein (Gs) [1] [3].

TFLLRNPNDK-NH2 is a biologically active peptide and a thrombin receptor activating peptide (TRAP). As a PAR-1 agonist, it reversibly binds to PAR-1, mimicking the 'tethered ligand' created by thrombin through proteolytic substrate cleavage. It also induces increased liquid and protein permeability, similar to thrombin's effect.

Heteropodatoxin-1 (HpTx1), a spider peptide toxin, acts as an inhibitor of the Kv4.2 current, while concurrently inhibiting Nav1.7 and activating Nav1.9 channels. However, it has no effect on Nav1.8 channels [1].

LAU-0901, a platelet-activating factor (PAF) receptor antagonist, demonstrates efficacy in reducing infarct volume and enhancing neurological function in rats subjected to middle cerebral artery occlusion (MCAO)-induced cerebral ischemia, at doses of 30, 60, and 90 mg/kg. Furthermore, it diminishes microglial infiltration while promoting astrocytic and neuronal survival in the same model. Additionally, at a dose of 30 mg/kg, LAU-0901, either alone or combined with atorvastatin, shows a capability to inhibit tumor growth in a U87MG glioblastoma mouse orthotopic tumor model.

Lys-γ3-MSH(human) TFA, a melanocortin peptide originating from the C-terminal fragment of pro-opiomelanocortin (POMC), enhances the steroidogenic response of rat adrenal glands to adrenocorticotrophin (ACTH). It is a potent stimulator of lipolysis, demonstrating an apparent EC50 of 3.56 nM, by activating hormone-sensitive lipase (HSL) and Perilipin A, leading to lipolysis [1] [2].

EGFRvIII peptide, a synthetic peptide mirroring the EGFRvIII fusion junction—a tumor-specific, perpetually active EGFR variant missing amino acids 6-273 of the wild-type—binds to HLA-A*0201-positive T2 cells under MHC class I at 25 µg/ml. It enables antigen presentation in dendritic cells from human peripheral blood mononuclear cells (PBMCs), thus activating CD8+ cytotoxic T lymphocytes and prompting IFN-γ production. Administered at 15 µg/animal with the TLR5 agonist flagellin B, EGFRvIII peptide elevates CD8+ T cell numbers, lowers regulatory T cells (Tregs) in the brain, diminishes tumor volume, and extends survival in a GL261 glioblastoma mouse model.

CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist, capable of activating the kappa opioid receptor with an EC50 value of 10.9 nM. It is utilized in the research of peripheral pain.

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA acts as a specific agonist for the neuropeptide Y Y1 receptor, while also activating receptors Y4 and Y5. This compound is known to elevate blood pressure in anesthetized rats and enhance food intake [1] [2].

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.

TAT-CIRP, a trans-activating (Tat) cold-inducible RNA-binding protein-derived peptide, functions as an inhibitor of myeloid differentiation protein 2 (MD2). It has demonstrated significant neuroprotective effects against ischemic and hemorrhagic stroke in mouse models [1].

YFLLRNP is a biologically active peptide functioning as a partial agonist of PAR-1, selectively activating the G12/13 signaling pathway. At low concentrations, YFLLRNP (60 μM) does not activate Gq or Gi pathways.

Peptide 401 is an antimicrobial peptide (AMP) derived from the venom of bees and wasps. Peptide 401 induces mast cell degranulation, activating histamine release from peritoneal mast cells. Additionally, peptide 401 exhibits some anti-inflammatory activit

Cenderitide, a natriuretic peptide (NP) that combines C-type natriuretic peptide (CNP) with the C-terminus of Dendroaspis natriuretic peptide (DNP), serves as a potent agonist of the particulate guanylyl cyclase receptor (pGC). By activating both pGC-A and pGC-B receptors, it stimulates the production of the second messenger cGMP, suppresses aldosterone, and maintains glomerular filtration rate (GFR) without affecting blood pressure. This compound is particularly significant in the context of heart failure research, as evidenced by references [1] [2] [3].

γ-1-Melanocyte Stimulating Hormone (MSH), amide, a peptide consisting of 11 amino acids, plays a critical role in regulating sodium (Na+) balance and blood pressure by activating melanocortin receptor 3 (MC3-R).

Calcitonin Gene-Related Peptide (CGRP) II, rat TFA, functions as a potent and enduring vasodilator by activating CGRP receptors. This compound is utilized in cardiovascular disease research [1].

pTH-Related Protein (1-40) (human, mouse, rat) enhances calcium absorption in rat intestinal cells by activating the PTHR1 receptor and the PKCα/β signaling pathways. This compound also increases the expression of the parathyroid hormone 1 receptor (PTHR1) and four key proteins involved in transcellular calcium transport: potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium Exchanger 1 (NCX1), and plasma membrane calcium ATPase 1 (PMCA1) [1].

MMK1 TFA is a potent, selective agonist for the human formyl peptide receptor like-1 (FPRL-1/FPR2), exhibiting EC50 values of <2 nM for FPRL-1 and >10,000 nM for FPR1. This compound acts as a powerful chemotactic and calcium-mobilizing agent, effectively activating phagocytic leukocytes. It significantly enhances the Pertussis Toxin-sensitive production of proinflammatory cytokines IL-1b and IL-6 by human monocytes. Additionally, MMK1 TFA has been demonstrated to exhibit anxiolytic-like activity [1] [2] [3] [4].

PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in normal human pancreas and adrenal gland tissue and in some tumors that produce vasoactive intestinal peptide (VIP). PRP (1-29) is secreted by CHO-K1 cells that express human recombinant preproPACAP.

Phoenixin-14 (PNX-14), an active endogenous isoform, induces an anxiolytic effect by activating the AHA GnRH system in mice and protects against ischemia/reperfusion-induced cytotoxicity in microglia [1] [2].

Ac9-25 TFA, an N-terminal peptide of Annexin I, functions as a formyl peptide receptor (FPR) agonist, activating neutrophil NADPH oxidase via FPR [1] [2].

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

Rusalatide acetate (TP508 amide acetate), a regenerated peptide, alleviates radiation-induced gastrointestinal injury by activating stem cells and protecting recess integrity.

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.