Neuropeptide-Y-Receptor-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Neuropeptide HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Y HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:

2、/www.MedChemE/Targets/Neuropeptide Y Receptor.html ReceptorNPY receptorNeuropeptide Y receptors belong G protein-coupled receptor superfamily and comprise various subtypes. There are currently fivecloned NPY receptor subtypes in mammals, termed Y1, Y2, Y4, Y5, and Y6. Neuropeptide Y receptors mediat

3、e a variety ofphysiological responses including feeding and vasoconstriction.Subtypes Y1, Y2, Y4 and Y5 are expressed in humans. They are present mainly in the central and peripheral nervous systems as wellas other tissues, such as the cardiovascular system. Their physiologic ligands are the neurotr

4、ansmitter Neuropeptide Y and the 2hormones peptide YY (PYY) and pancreatic polypeptide (PP).Neuropeptide Y and its receptors regulate important biological and pathophysiological functions, such as blood pressure,neuroendocrine secretions, seizures, neuronal excitability and neuroplasticity.www.MedCh

5、emE 1 HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Neuropeptide HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Y HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK h

6、ttps:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.Med

7、ChemE/Targets/Neuropeptide Y Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.MedChemE/Ta

8、rgets/Neuropeptide Y Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neuropeptide Y Receptor.html Modulators HYPERLINK https:/www.MedChemE/r-jnj-31020028.html (R)-JNJ-31020028 HYPERLINK https:/www.MedChemE/r-jnj-31020028.html H

9、YPERLINK https:/www.MedChemE/bibo3304-tfa.html BIBO3304 HYPERLINK https:/www.MedChemE/bibo3304-tfa.html HYPERLINK https:/www.MedChemE/bibo3304-tfa.html TFACat. No.: HY-107479 Cat. No.: HY-107725(R)-JNJ-31020028 is a high affinity, selectivebrain penetrant neuropeptide Y Y2 receptorantagonist, with p

10、IC values of 8.07, 8.22 and508.21 for human, rat, and mouse Y2 receptor,respectively.BIBO3304 TFA is a potent, orally active, andselective neuropeptide Y (NPY) Y1 receptorantagonist, with subnanomolar affinity for boththe human and the rat Y1 receptor (IC =0.38 and500.72 nM, respectively).Purity: 98

11、%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.95%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/bibp3226.html BIBP3226 HYPERLINK https:/www.MedChemE/bibp3226.html HYPERLINK https:/www.MedChemE/bibp3226-tfa.html BIBP3226 HYPERLI

12、NK https:/www.MedChemE/bibp3226-tfa.html HYPERLINK https:/www.MedChemE/bibp3226-tfa.html TFACat. No.: HY-107726A Cat. No.: HY-107726BIBP3226 is a potent and selective neuropeptide YY1 (NPY Y1) and neuropeptide FF (NPFF)receptor antagonist, with Ks of 1.1, 79, and 108inM for rNPY Y1, hNPFF2, and rNPF

13、F, respectively.BIBP3226 displays anxiogenic-like effect.BIBP3226 TFA is a potent and selectiveneuropeptide Y Y1 (NPY Y1) and neuropeptide FF(NPFF) receptor antagonist, with Ks of 1.1, 79,iand 108 nM for rNPY Y1, hNPFF2, and rNPFF,respectively. BIBP3226 TFA displaysanxiogenic-like effect.Purity: 98%

14、Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.09%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/BIIE-0246.html BIIE-0246(AR-H 053591) Cat. No.: HY-101986 HYPERLINK https:/www.MedChemE/bms-193885.html BMS-193885Cat. No.: HY-

15、120619BIIE-0246 is a potent and highly selectivenon-peptide neuropeptide Y (NPY) Y receptor2antagonist, with an IC of 15 nM.50Purity: 99.0%Clinical Data: No Development ReportedSize: 1 mgBMS-193885 is a potent, selective, competitive,and brain penetrant neuropeptide Y receptor1antagonist with a Ki o

16、f 3.3 nM, and has an IC50 of5.9 nM for hY , which displays 100, 1160, 160 and 160-fold selectivity over , hY , hY and hY receptors, respectively .1 2 4 5Purity: 99.08%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cart-55-102-human-tfa.html CART(55-

17、102)(human) HYPERLINK https:/www.MedChemE/cart-55-102-human-tfa.html HYPERLINK https:/www.MedChemE/cart-55-102-human-tfa.html TFA HYPERLINK https:/www.MedChemE/cart-55-102-human-tfa.html HYPERLINK https:/www.MedChemE/cart-55-102-rat-tfa.html CART(55-102)(rat) HYPERLINK https:/www.MedChemE/cart-55-10

18、2-rat-tfa.html HYPERLINK https:/www.MedChemE/cart-55-102-rat-tfa.html TFACat. No.: HY-P1304A Cat. No.: HY-P1305ACART(55-102)(human) TFA is a human satiety factorwith potent appetite-suppressing activity.CART(55-102)(human) TFA is closely associated withleptin and neuropeptide Y.CART(55-102)(rat) TFA

19、 is a rat satiety factor withpotent appetite-suppressing activity.CART(55-102)(rat) TFA is closely associated withleptin and neuropeptide Y. CART(55-102)(rat) TFAcan induces anxiety and stress-related behavior.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data:

20、 No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CGP71683_hydrochloride.html CGP71683 HYPERLINK https:/www.MedChemE/CGP71683_hydrochloride.html HYPERLINK https:/www.MedChemE/CGP71683_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/CGP71683_hydrochloride.html HYPE

21、RLINK https:/www.MedChemE/cym-9484.html CYM HYPERLINK https:/www.MedChemE/cym-9484.html HYPERLINK https:/www.MedChemE/cym-9484.html 9484(CGP71683A) Cat. No.: HY-107723Cat. No.: HY-107735CGP71683 hydrochloride is a competitiveneuropeptide Y5 receptor antagonist with a K ofi1.3 nM, and shows no obviou

22、s activity at Y1receptor (K, 4000 nM) and Y2 receptor ( ,i Ki200 nM) in cell membranes.CYM 9484 is a selective and highly potentneuropeptide Y (NPY) Y2 receptor antagonist withan IC value of 19 nM.50Purity: 99.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurit

23、y: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/cym2503.html CYM2503 HYPERLINK https:/www.MedChemE/cym2503.html HYPERLINK https:/www.MedChemE/Benzo3,4cyclohept1,2-dimidazole,_1,4,5,6-t

24、etrahydro-9-methyl-2-_3-pyridinyl_-.html FR252384Cat. No.: HY-123671 Cat. No.: HY-U00335CYM2503 is a putative GalR2-positive allostericmodulator. CYM2503 increases the latency to firstelectrographic seizure and decreases the totaltime in seizure. CYM2503 also attenuateselectroshock-induced seizures

25、in mice.FR252384 is a neuropeptide Y-Y5 receptorantagonist, with an IC of 2.3 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html Galanin HYPERLIN

26、K https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html (1-16), HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html mouse, HYPERLINK htt

27、ps:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html porcine, HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html rat HYPERLINK https:/www

28、.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html Galanin HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html (1-16), HYPERLINK ht

29、tps:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html mouse, HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html porcine,

30、HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html rat HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html HYPERLINK https:/www.MedChemE/Galanin_1-16_,_mouse,_porcine,_rat_TFA.html

31、TFACat. No.: HY-P1578 Cat. No.: HY-P1578AGalanin (1-16), mouse, porcine, rat is an agonistof the hippocampal galanin receptor, with a Kdof 3 nM.Galanin (1-16), mouse, porcine, rat (TFA) is anagonist of the hippocampal galanin receptor, witha K of 3 nM.dPurity: 98%Clinical Data: No Development Report

32、edSize: 1 mg, 5 mgPurity: 99.39%Clinical Data: No Development ReportedSize: 500 g, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse.html Galanin HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse.html HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse.html (1-29)(rat, HYPERLINK ht

33、tps:/www.MedChemE/galanin-1-29-rat-mouse.html HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse.html mouse) HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse.html HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse-tfa.html Galanin HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse-tfa.html

34、 HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse-tfa.html (1-29)(rat, HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse-tfa.html HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse-tfa.html mouse) HYPERLINK https:/www.MedChemE/galanin-1-29-rat-mouse-tfa.html HYPERLINK https:/www.MedChemE/ga

35、lanin-1-29-rat-mouse-tfa.html TFACat. No.: HY-P1132 Cat. No.: HY-P1132AGalanin (1-29)(rat, mouse) is a non-selectivegalanin receptor agonist, with Ks of 0.98, 1.48iand 1.47 nM for GAL1, GAL2 and GAL3 respectively.Anticonvulsant effect.Galanin (1-29)(rat, mouse) TFA is a non-selectivegalanin receptor

36、 agonist, with Ks of 0.98, 1.48iand 1.47 nM for GAL1, GAL2 and GAL3, respectively.Anticonvulsant effect.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Galanin_1-30_,_human.html Galanin H

37、YPERLINK https:/www.MedChemE/Galanin_1-30_,_human.html HYPERLINK https:/www.MedChemE/Galanin_1-30_,_human.html (1-30), HYPERLINK https:/www.MedChemE/Galanin_1-30_,_human.html HYPERLINK https:/www.MedChemE/Galanin_1-30_,_human.html human HYPERLINK https:/www.MedChemE/Galanin_1-30_,_human.html HYPERLI

38、NK https:/www.MedChemE/galanin-receptor-ligand-m35.html Galanin HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35.html HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35.html Receptor HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35.html HYPERLINK https:/www.MedChemE/galanin-

39、receptor-ligand-m35.html Ligand HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35.html HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35.html M35Cat. No.: HY-P1127 Cat. No.: HY-P1840Galanin (1-30), human is a 30-amino acidneuropeptide, and acts as an agonist of GalR1 andGalR2 recepto

40、rs, with Ks of both 1 nM.iGalanin Receptor Ligand M35 is a high-affinityligand and antagonist of galanin receptor(K =0.1 nM). Galanin Receptor Ligand M35 exertsda K values of 0.11 and 2.0 nM for human galaninireceptor type 1 and 2, respectively.Purity: 99.11%Clinical Data: No Development ReportedSiz

41、e: 500 g, 1 mg, 5 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html Galanin HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.

42、html Receptor HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html Ligand HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html M35 HYPERLI

43、NK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html TFA HYPERLINK https:/www.MedChemE/galanin-receptor-ligand-m35-tfa.html HYPERLINK https:/www.MedChemE/Galantide.html GalantideCat. No.: HY-P1840A Cat. No.: HY-P0262Galanin Re

44、ceptor Ligand M35 TFA is a high-affinityligand and antagonist of galanin receptor (K =0.1dnM). Galanin Receptor Ligand M35 TFA exerts a Kivalues of 0.11 and 2.0 nM for human galaninreceptor type 1 and 2, respectively.Galantide, a non-specific galanin receptorantagonist, is a peptide consisting of fr

45、agmentsof galanin and substance P. Galantide recognizestwo classes of galanin binding sites (K 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.27%Clinical Data: No Development ReportedSize: 500 g, 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/galnon.html GalnonCat. No.:

46、HY-103536 HYPERLINK https:/www.MedChemE/gr231118.html GR231118(1229U91; GW1229) Cat. No.: HY-P1321Galnon is a selective and non-peptide agonist ofgalanin GAL1 and GAL2 receptor, with Ks of 11.7iand 34.1 M respectively. Galnon exhibitsanticonvulsant and anxiolytic effects.GR231118, an analogue of the

47、 C-terminus ofneuropeptide Y, is a potent , competitive andrelative seletive antagonist at human neuropeptideY Y receptor with a pK of 10.4.iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChem

48、E/gr231118-tfa.html GR231118 HYPERLINK https:/www.MedChemE/gr231118-tfa.html HYPERLINK https:/www.MedChemE/gr231118-tfa.html TFA(1229U91 TFA; GW1229 TFA) Cat. No.: HY-P1321A HYPERLINK https:/www.MedChemE/HT-2157.html HT-2157(SNAP 37889) Cat. No.: HY-100717GR231118 TFA, an analogue of the C-terminus

49、ofneuropeptide Y, is a potent , competitive andrelative seletive antagonist at human neuropeptideYY receptor with a pK of 10.4.iHT-2157 (SNAP 37889) is a selective,high-affinity, competitive antagonists of galanin-3receptor (Gal ).3Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPur

50、ity: 98.0%Clinical Data: Phase 2Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/JNJ-31020028.html JNJ-31020028 HYPERLINK https:/www.MedChemE/JNJ-31020028.html HYPERLINK https:/www.MedChemE/jnj-5207787.html JNJ-5207787Cat. No.: HY-14450 Cat. No.: HY-107732JNJ-31020028

51、 is a selective brain penetrantantagonist of neuropeptide Y2 receptor with highaffinity (pIC50=8.07, human; pIC50=8.22 rat);100-fold selective versus human Y1/Y4/Y5receptors.Purity: 98.62%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgJNJ-5207787 is a nonpeptidic,

52、selective andpenetrate the blood-brain barrier neuropeptide YY receptor (Y ) antagonist. JNJ-52077872 2inhibits the binding of peptide YY (PYY) withpIC s of 7.0 and 7.1 for human Y receptor and50 2rat Y receptor, respectively.2Purity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPER

53、LINK https:/www.MedChemE/l-152804.html L HYPERLINK https:/www.MedChemE/l-152804.html HYPERLINK https:/www.MedChemE/l-152804.html 152804 HYPERLINK https:/www.MedChemE/l-152804.html HYPERLINK https:/www.MedChemE/lu-aa33810.html Lu HYPERLINK https:/www.MedChemE/lu-aa33810.html HYPERLINK https:/www.MedC

54、hemE/lu-aa33810.html AA33810Cat. No.: HY-107734 Cat. No.: HY-107729L 152804 is an orally active and selectiveneuropeptide Y Y5 receptor (NPY5-R) antagonist,with a K of 26 nM for . L 152804 causesi hY5weight loss in diet-induced obese mice bymodulating food intake and energy expenditure.Lu AA33810 is

55、 a potent and selective antagonist ofneuropeptide Y5 receptor with a K of 1.5 nM forithe human receptor. Lu AA33810 exhibtsantianxiolytic-like and antidepressant-likeeffects.Purity: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No D

56、evelopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/m1145.html M1145 HYPERLINK https:/www.MedChemE/m1145.html HYPERLINK https:/www.MedChemE/m1145-tfa.html M1145 HYPERLINK https:/www.MedChemE/m1145-tfa.html HYPERLINK https:/www.MedChemE/m1145-tfa.html TFACat. No.: HY-P1135 Cat. No.: HY-

57、P1135AM1145, a chimeric peptide, is a selective galaninreceptor type 2 (GAL2) agonist, with a K of 6.55inM. M1145 shows more than 90-fold higher affinityfor GAL2 over GAL1 (K =587 nM) and a 76-fold higheriaffinity over GalR3 (K=497 nM).iM1145 TFA, a chimeric peptide, is a selectivegalanin receptor t

58、ype 2 (GAL2) agonist, with a Kiof 6.55 nM. M1145 TFA shows more than 90-foldhigher affinity for GAL2 over GAL1 (K =587 nM) andia 76-fold higher affinity over GalR3 (K=497 nM).iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg

59、, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/M40.html M40 HYPERLINK https:/www.MedChemE/M40.html HYPERLINK https:/www.MedChemE/m617.html M617Cat. No.: HY-P1025 Cat. No.: HY-P1131M40 is a potent, non-selective galanin receptorantagonist.M617 is a sele

60、ctive galanin receptor 1 (GAL1)agonist, with Ks of 0.23 and 5.71 nM for GAL1 andiGAL2, respectively. M617, acting through itscentral GAL1, can promote GLUT4 expression andenhance GLUT4 content in the cardiac muscle oftype 2 diabetic rats.Purity: 98%Clinical Data: No Development ReportedSize: 500 g,