npy

neuropeptide Y Y5 receptor antagonist

Neuropeptide Y (scrambled) Acetate (Pro-Neuropeptide Y (scrambled) Acetate) is a scrambled peptide of Neuropeptide Y that has been implicated in Alzheimer's disease (AD) and may have neuroprotective effects.

[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent, selective neuropeptide Y Y5 receptor agonist, demonstrating binding affinity with an IC50 of 0.24 nM for the hY5 receptor. This compound significantly stimulates food intake [1].

Fenpyroximate is an acaricide and insecticide. It blocking the mitochondrial electron transport in complex I.

Tebufenpyrad (Comanche) (mitochondrial complex-1 inhibitors) is an agro-chemically important acaricide that functions like the known mitochondrial toxicant rotenone.

Neuropeptide Y (NPY), a neuropeptide, plays roles in regulating appetite, vasoconstriction, cardiac contractility, and intestinal secretion, acting as an agonist for NPY receptors Y1, Y2, and Y5. Expressed ubiquitously, NPY modulates cellular responses by selectively inhibiting forskolin-induced cAMP accumulation in L-M(TK-) cells expressing rat Y1 or Y2 and in HEK293 cells expressing rat Y5, more so than in cells expressing rat Y4 receptors (EC50s = 0.15, 2.7, 0.66, and >1,000 nM, respectively). Additionally, it elevates perfusion pressure in isolated guinea pig hearts (EC30 = 1.3 nM) and, when administered intracerebroventricularly at 300 pmol/animal, it notably increases food intake in rats.

Tolfenpyrad is an effective insecticide[1], used against pests that are resistant to existing insecticides such as organophosphates and carbamates.[2]

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

Pancreatic Polypeptide (human) acetate is a C-terminally amidated 36 amino acid peptide, which acts as a neuropeptide Y (NPY) Y4/Y5 receptor agonist.

BWX 46 Acetate is a potent, highly selective neuropeptide Y (NPY) receptor agonist with IC50 of 0.5 nM.

Galanin (1-16), mouse, porcine, rat is a hippocampal galanin receptor agonist(Kd = 3 nM) with high biological activity on locus coeruleus neurons.

PACAP-38 (31-38), human, mouse, rat acetate is an activator of PAC1 receptor. PACAP-38 (31-38), human, mouse, rat acetate demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production and can

Peptide YY (PYY) (3-36), human (Peptide YY (3-36)) is a gut hormone peptide. Peptide YY (PYY) (3-36), human acts as a Y2 receptor agonist to reduce appetite.

Pancreatic Polypeptide, rat acetate is an agonist of NPY receptor, with high affinity at NPYR4.

[D-Trp34]-Neuropeptide Y Acetate is a potent and selective agonist of neuropeptide Y (NPY) Y5 receptor. [D-Trp34]-Neuropeptide acetate Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y Acetate markedly increases food intake in rats.

Potent, selective peptide agonist for the neuropeptide Y Y5 receptor (IC50 values for inhibition of NPY binding to human Y5, Y1, Y2 and Y4 receptors are 0.24, 530, > 500, and 51 nM respectively, Ki at Y5 = 0.1 - 0.15 nM). Stimulates food intake in vivo.

Mefenpyr-diethyl is an herbicide safener, which protects crops against herbicide injury.

Sulfinpyrazone (NSC-75925) is a uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.

Nitenpyram (Capstar) is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.

Phenchlobenpyrrone has potential as a treatment for Alzheimer's disease.

TAT (47-57) GGG-Cys(Npys) is a cell-penetrating peptide (CPP) with potential applications in intracellular drug delivery research [1].

(Rac)-Benpyrine is a potent and orally active inhibitor of TNF-α.

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abolishes the TNF-α-induced nuclear translocation of NF-κB/p65 in RAW264.7 cells[1].Benpyrine only blocks cell death induced by TNF-αWT and Y119A, and increases the cell survival rate up to 80%. Benpyrine does not obviously affect L57A- and Y59L-induced cytotoxicity in L929 cells[1]. Benpyrine (25-50 mg/kg; oral gavage; daily; for 2 weeks; Balb/c mice) treatment significantly relieves the symptoms of collagen-induced arthritis. Benpyrine dose-dependently decreases the levels of proinflammatory cytokines, such as IFN-γ, IL-1β and IL-6, and increases the concentration of the anti-inflammatory cytokine IL-10[1].Endotoxemia murine model shows that Benpyrine (25 mg/kg) could attenuate TNF-α-induced inflammation, thereby reducing liver and lung injury[1]. [1]. Weiguang Sun, et al. Discovery of an Orally Active Small Molecule TNF-α Inhibitor. J Med Chem. 2020 Jul 15.

Cys(Npys)-TAT (47-57), a peptide fragment corresponding to the transduction domain of the TAT peptide, features an activated cysteine residue C and is capable of electrostatically interacting with plasmid DNA. Notably, TAT is a small nuclear transcriptional activator protein encoded by HIV-1 [1].

BIBO3304 is a selective NPY Y1 receptor antagonist (IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively). BIBO3304 inhibits NPY- and fasting-induced feeding in vivo following central administration.

High affinity neuropeptide Y Y1 receptor agonist

Potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses

Potent neuropeptide Y (NPY) Y5 receptor agonist (pEC50 values are 7.82, 6.28, 6.44 and > 6 at rat Y5, Y4, Y1 and Y2 receptors respectively) that displays > 26-fold, > 1000-fold and > 1000-fold selectivity over Y1, Y2 and Y4 receptors respectively. Induces

Neuropeptide Y (3-36) (human, rat) is a metabolite of neuropeptide Y (NPY) generated by dipeptidyl peptidase-4 (DPP4). Known as a selective Y2 receptor agonist, Neuropeptide Y (3-36) (human, rat) effectively reduces the release of norepinephrine via the Y2 receptor[1][2].

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

BIBO3304 (diTFA), a selective neuropeptide Y (NPY) Y1 receptor antagonist, demonstrates oral efficacy. It exhibits high affinity for Y1 receptors in both humans and rats, with IC50 values of 0.38 nM and 0.72 nM, respectively. Additionally, BIBO3304 (diTFA) enhances bone-tendon healing via the Wnt/β-catenin signaling pathway [1] [2] [3].

[D-Arg25]-Neuropeptide Y (human) ([D-Arg25] NPY), a Y1 receptor selective agonist, plays a role in Alzheimer's disease (AD) and safeguards rat cortical neurons from β-Amyloid toxicity [1].

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.

BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist. With an IC50 of 15 nM.

LU AA33810 is a neuropeptide Y (NPY) Y5 receptor antagonist.

HT-2157 (SNAP-37889) is a selective, high-affinity competitive antagonist of the galanin-3 receptor (Gal3), demonstrating effective inhibition of this target.

Neuropeptide Y (3-36) (porcine) acts as an agonist for the Y2 subtype of the neuropeptide Y (NPY) receptor, effectively stimulating feeding behavior in rats. This compound exhibits high selectivity for the Y2 receptor compared to the non-selective Y1/Y2 receptor ligand, Neuropeptide Y 1-36 [1] [2] [3].

Velneperit (S2367) is potent and selective neuropeptide Y (NPY) Y5 receptor under evaluating for treatment of obesity.

JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22, rat); it exhibits >100-fold selectivity for Y2 versus human Y1/Y4/Y5 receptors.

GW438014A is a selective NPY-Y5 receptor antagonist.

BIBO3304 TFA is an effective, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist (IC50:0.38 and 0.72 nM for the human and the rat Y1 receptor).

CGP71683 hydrochloride (CGP71683A) is a competitive neuropeptide Y5 receptor antagonist (Ki: 1.3 nM) and shows no obvious activity at Y1 receptor (Ki >4000 nM) and Y2 receptor (Ki: 200 nM) in cell membranes.

Positive allosteric modulator of neuropeptide Y receptor 4 (Y4R). Potentiates Y4R response to pancreatic polypeptide (PP), neuropeptide Y (NPY) and peptide YY (PYY) (EC50 values are 0.03, 0.4 and 0.5 nM respectively). Shows selectivity for Y4R over Y1R, Y2R and Y5R. Schubert et al (2017) Identification and characterization of the first selective Y4 receptor positive allosteric modulator. J.Med.Chem. 60 7605 PMID:28795803

Potent, selective and competitive nonpeptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM). Displays > 650-fold selectivity for NPY Y2 over Y1, Y4 and Y5 receptors. Active in vivo.

Neuropeptide Y (18-36) (porcine) acts as a competitive antagonist of the neuropeptide Y (NPY) cardiac receptor, effectively blocking the attachment of I-NPY to cardiac ventricular membranes. Its action is concentration-dependent, exhibiting an IC50 value of 158 nM and a Ki value of 140 nM. This compound is utilized in the study of congestive heart failure [1].

Neuropeptide Y (22-36), a 15 amino acid peptide, is a fragment of Neuropeptide Y.Neuropeptide Y (NPY) is a 36 amino-acid neuropeptide that is involved in various physiological and homeostatic processes in both the central and peripheral nervous systems. N

Agouti-related peptide (AgRP) is a neuropeptide produced in the brain by the AgRP/NPY neuron. It is only synthesized in NPY containing cell bodies located in the ventromedial part of the arcuate nucleus in the hypothalamus. The appetite-stimulating effect

PACAP-38 (16-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production.

Galnon is a galanin receptor agonist, improves intrinsic cortical bone tissue properties

NTNCB hydrochloride is an antagonist of neuropeptide Y (NPY) Y5 receptor.