NPY Y2 receptor
NPY Y2 receptor is a widely distributed Gi/Go-coupled GPCR that inhibits adenylate cyclase, reduces cAMP accumulation, and modulates Ca2+/K+ channel signaling[1][2]. Mechanistically, Y2 signaling supports presynaptic inhibition by neuropeptide Y (NPY) and peptide YY (PYY), linking receptor activation to reduced neuronal excitability and regulated neurotransmitter release[1][3]. In disease models, Y2 receptor biology connects to feeding control, anxiety-related behavior, epilepsy research, neuroblastoma, and obesity-relevant experimental designs[1][4]. Compared with related isoforms, Y2 receptor selectivity depends on ligand structure and receptor subtype pharmacology, distinguishing it from Y1, Y4, and Y5 receptors in assay design[2][5]. For experimental applications, Y2-selective agonists can inhibit food intake and promote fat metabolism in mice, while nonpeptidic Y2 antagonists such as SF-11 provide brain-penetrant tools for behavioral studies[4][6].- Y2 receptor assays should prioritize Gi/Go signaling, cAMP inhibition, and subtype-selective ligand validation[2][5].- Feeding, anxiety, epilepsy, and neuroblastoma models provide practical contexts for NPY2R study[1][4].- Agonists and antagonists support mechanistic experiments when receptor selectivity is experimentally confirmed[5][6].
References:
- [1]. Parker SL, et al. Neuropeptide Y Y2 receptor in health and disease. Br J Pharmacol. 2008 Feb;153(3):420-31. [Content Brief]
- [2]. Pedragosa-Badia X, et al. Neuropeptide Y receptors: how to get subtype selectivity. Front Endocrinol (Lausanne). 2013 Feb 4;4:5. [Content Brief]
- [3]. Kang H, et al. Structural basis for Y2 receptor-mediated neuropeptide Y and peptide YY signaling. Structure. 2023 Jan 5;31(1):44-57.e6. [Content Brief]
- [4]. Balasubramaniam A, et al. Neuropeptide Y (NPY) Y2 receptor-selective agonist inhibits food intake and promotes fat metabolism in mice: combined anorectic effects of Y2 and Y4 receptor-selective agonists. Peptides. 2007 Feb;28(2):235-40. [Content Brief]
- [5]. Mittapalli GK, et al. Ligands of the neuropeptide Y Y2 receptor. Bioorg Med Chem Lett. 2014 Jan 15;24(2):430-41. [Content Brief]
- [6]. Domin H, et al. Characterization of the Brain Penetrant Neuropeptide Y Y2 Receptor Antagonist SF-11. ACS Chem Neurosci. 2019 Aug 21;10(8):3454-3463. [Content Brief]
-
NPY Y2 receptor Related Products (23)
Related Products (23)
- 1
- 2
-
BIIE-0246
0 ImagesSynonyms: AR-H 053591BIIE-0246 (AR-H 053591) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [125I]PYY3-36. BIIE-0246 decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 reduces albuminuria in ADR nephropathy.
-
Peptide YY (PYY) (3-36), Human
0 ImagesPeptide YY (PYY) (3-36), Human is an endogenous appetite-suppressing peptide that acts as a selective agonist of neuropeptide Y (NPY) Y2 receptor. Peptide YY (PYY) (3-36), Human inhibits intestinal fluid secretion, colonic propulsion, and reduces fecal output in mouse models. Peptide YY (PYY) (3-36), Human inhibits dmPGE2-, 5HT (HY-B1473A)-, and Castor oil (HY-107799)-induced diarrhea in mice. Peptide YY (PYY) (3-36), Human improves metabolic parameters and mitochondrial function in obese rat MASLD models. Peptide YY (PYY) (3-36), Human can be used for research on intestinal diseases such as diarrhea and metabolic dysfunction-associated steatotic liver disease.
-
RF9
0 ImagesRF9 is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.
-
Neuropeptide Y (3-36) (human, rat)
0 ImagesCat. No.: HY-P2543CAS No.: 150138-78-6Neuropeptide Y (3-36) (human, rat) is a neuropeptide Y fragment derived from humans or rats. Neuropeptide Y is an extremely abundant neurotransmitter in central and peripheral neurons, and it participates in the regulation of psychomotor activity, circadian rhythm, feeding behavior and cardiovascular function. Neuropeptide Y (3-36) (human, rat) can serve as a substrate to be sequentially degraded from its N-terminus by AfuS28, and it requires binding to AfuS28 and SedB to be decomposed into amino acids, dipeptides and tripeptides[1][2].
-
Neuropeptide Y (13-36), amide, human
0 ImagesSynonyms: Neuropeptide Y (13-36), humanNeuropeptide Y (13-36), amide, human is a selective neuropeptide Y2 receptor agonist.
-
NNC0165-1273 TFA
0 ImagesCat. No.: HY-P11291ANNC0165-1273 TFA is a selective NPY Y2 receptor agonist with a Ki of 2 nM and an EC50 of 5.0 nM. NNC0165-1273 TFA blocks Ghrelin-induced cFos expression. NNC0165-1273 TFA reduces nocturnal food intake, attenuates feeding behavior, induces early satiety, and causes dose-dependent decreases in body weight and fat mass in diet-induced obese mice. When used in combination with Semaglutide (HY-114118), NNC0165-1273 TFA reduces preference for high-fat diet, promotes body weight loss, and produces sustained weight loss effects in diet-induced obese rats. NNC0165-1273 TFA can be used in studies related to diet-induced obesity.
-
NNC0165-1273
0 ImagesCat. No.: HY-P11291NNC0165-1273 is a selective NPY Y2 receptor agonist with a Ki of 2 nM and an EC50 of 5.0 nM. NNC0165-1273 blocks Ghrelin-induced cFos expression. NNC0165-1273 reduces nocturnal food intake, attenuates feeding behavior, induces early satiety, and causes dose-dependent decreases in body weight and fat mass in diet-induced obese mice. When used in combination with Semaglutide (HY-114118), NNC0165-1273 reduces preference for high-fat diet, promotes body weight loss, and produces sustained weight loss effects in diet-induced obese rats. NNC0165-1273 can be used in studies related to diet-induced obesity.
-
CYM 9484
0 ImagesCYM 9484 is a selective and highly potent neuropeptide Y (NPY) Y2 receptor antagonist with an IC50 value of 19 nM.
-
SF 11
0 ImagesSF 11 is a potent and brain penetrant neuropeptide Y Y2 receptor antagonist (IC50=199 nM). Antidepressant-like activity.
-
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide
![[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide](https://file.medchemexpress.com/product_pic/hy-p1324.gif "Click to View [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide Product Detail")
0 Images[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.
-
(Leu31,Pro34)-Peptide YY (human) TFA
0 ImagesCat. No.: HY-P3877APurity: 98.63%(Leu31,Pro34)-Peptide YY (human) (TFA) is the TFA form of (Leu31,Pro34)-Peptide YY (human) (HY-P3877). (Leu31,Pro34)-Peptide YY (human) (TFA) is a Peptide YY (HY-P1514) derivative and is a potent and selective Y1 agonist with a KD of 1.0 nM.
-
JNJ-5207787
0 ImagesJNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors.
-
RF9 hydrochloride
0 ImagesCat. No.: HY-107382APurity: 99.91%RF9 hydrochloride is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.
-
(Leu31,Pro34)-Peptide YY (human)
0 ImagesCat. No.: HY-P3877CAS No.: 179986-95-9(Leu31,Pro34)-Peptide YY (human) is a Peptide YY (HY-P1514) derivative and is a potent and selective Y1 agonist with a KD of 1.0 nM.
-
GEP44
0 ImagesCat. No.: HY-P11043GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research.
-
BWX 46
0 ImagesCat. No.: HY-P1325CAS No.: 172997-92-1Synonyms: ((Cys31, Nva 34)-Neuropeptide Y (27-36))2BWX 46 (((Cys31, Nva 34)-Neuropeptide Y (27-36))2) is a selective Y5 receptor agonist with an IC50 value of 0.85 nM. BWX 46 can inhibit the synthesis of cAMP in Y5 cells.
-
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA
![[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA](https://file.medchemexpress.com/product_pic/hy-p1324a.gif "Click to View [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA Product Detail")
0 ImagesCat. No.: HY-P1324A[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.
-
Peptide YY (pig)
0 ImagesCat. No.: HY-P2703CAS No.: 81858-94-8Peptide YY (pig) is a 36 amino acid gastrointestinal peptide, can be isolated from porcine duodenum. Peptide YY (pig) decreases appetite and food-intake by activation of the Y2 receptor. Peptide YY (pig) is present mainly in pancreatic endocrine cells with effect on both intestinal motility and the cardiovascular system.
-
(R)-JNJ-31020028
0 ImagesCat. No.: HY-107479CAS No.: 1094873-17-2(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
-
NPY Y2 antagonist 2
0 ImagesCat. No.: HY-180406CAS No.: 1262495-12-4NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal.
- 1
- 2
