Melatonin-Receptor-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html Melatonin HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html ReceptorMelatonin receptors belong to the G protein-coupled receptor superfamily, which preferentially

2、couple to G proteins. Thei/omelatonin receptor subfamily is composed of three members in mammals: MT and MT , which are both binding to the1 2neurohormone melatonin with high affinity, and GPR50, which shows high sequence homology to MT and MT but does not bind1 2to melatonin or any other known liga

3、nd.MT and MT are involved in various biological functions including the regulation of biological rhythms, sleep, pain, retinal, neuronal1 2and immune functions. Alteration of melatonin receptor function or expression in humans is associated with depression,Alzheimers disease and type 2 diabetes.www.

4、MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html Melatonin HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html HYPERLINK https:/www.M

5、edChemE/Targets/Melatonin Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html Activators HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melatonin Recep

6、tor.html & HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melatonin Receptor.html Antagonists HYPERLINK https:/www.MedChemE/2-iodomelatonin.html 2-Iodomelatonin HYPERLINK https:/www.MedChemE/2-iodomelatonin.html HYPERLINK https:/www.MedChemE/4-p-p

7、dot.html 4-P-PDOTCat. No.: HY-101176 Cat. No.: HY-1006092-Iodomelatonin is a potent agonist ofmelatonin receptor 1 (MT1) with a K valueiof 28 pM, it is more 5-fold selective for MT1over MT . 2-iodomelatonin can be used to2identify, characterize and localize melatoninbinding sites in the brain and pe

8、ripheral tissues.4-P-PDOT is a potent, selective and affinityMelatonin receptor (MT2) antagonist.4-P-PDOT is 300-fold more selective for MT2than MT1.Purity: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 99.45%Clinical Data: No Development ReportedSize: 10 mM 1

9、 mL, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/6-chloromelatonin.html 6-ChloromelatoninCat. No.: HY-100940 HYPERLINK https:/www.MedChemE/7-desmethyl-3-hydroxyagomelatine.html 7-Desmethyl-3-hydroxyagomelatine(3-Hydroxy-7-desmethyl agomelatine) Cat. No.: HY-1331126-Chloromelatonin is a potent melatonin

10、receptor agonist with greater metabolic stabilitythan melatonin. 6-Chloromelatonin compete for3H-melatonin and 2-125I-iodomelatoninbinding to MT1 receptors (pK=8.9 and 9.1,irespectively).7-Desmethyl-3-hydroxyagomelatine(3-Hydroxy-7-desmethyl agomelatine), a metaboliteof Agomelatine, has less activit

11、y thanAgomelatine. Agomelatine is a melatonergic(MT1 and MT2) agonist and serotonergic(5HT2C) antagonist.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/7-desmethyl-3-hydroxyagomelatine-d

12、3.html 7-Desmethyl-3-hydroxyagomelatine-d3(3-Hydroxy-7-desmethyl agomelatine-d3) Cat. No.: HY-133112S HYPERLINK https:/www.MedChemE/8-m-pdot.html 8-M-PDOT(AH-002) Cat. No.: HY-1013587-Desmethyl-3-hydroxyagomelatine-d3(3-Hydroxy-7-desmethyl agomelatine-d3) is thedeuterium labeled7-Desmethyl-3-hydroxy

13、agomelatine.8-M-PDOT (AH-002) is a selective melatonin MT2receptor agonist. 8-M-PDOT is 5.2-fold selectivefor MT2 over MT1 receptors. 8-M-PDOT bindshuman recombinant MT2 and MT2 receptors withpKi values of 8.23 and 8.95 respectively. 8-M-PDOThas anxiolytic-like activity.Purity: 98%Clinical Data: No

14、Development ReportedSize: 1 mg, 5 mgPurity: 98.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg HYPERLINK https:/www.MedChemE/ach-000143.html ACH-000143 HYPERLINK https:/www.MedChemE/ach-000143.html HYPERLINK https:/www.MedChemE/agomelatin-d3.html Agomelatin-d3Cat. No.: HY-138626(S-2

15、0098-d3) Cat. No.: HY-17038S2ACH-000143 is a potent and orally activemelatonin receptor agonist, with EC values50of 0.06 nM and 0.32 nM for MT1 and MT2,respectively.Agomelatin-d3 (S-20098-d3) is the deuteriumlabeled Agomelatine. Agomelatine (S-20098) is aspecific agonist of MT1 and MT2 receptorswith

16、 Ks of 0.1, 0.06, 0.12, and 0.27 nM foriCHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2,respectively.Purity: 98.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Agome

17、latine.html Agomelatine HYPERLINK https:/www.MedChemE/Agomelatine.html HYPERLINK https:/www.MedChemE/agomelatine-l_addition_-tartaric-acid.html Agomelatine HYPERLINK https:/www.MedChemE/agomelatine-l_addition_-tartaric-acid.html HYPERLINK https:/www.MedChemE/agomelatine-l_addition_-tartaric-acid.htm

18、l (L(+)-Tartaric HYPERLINK https:/www.MedChemE/agomelatine-l_addition_-tartaric-acid.html HYPERLINK https:/www.MedChemE/agomelatine-l_addition_-tartaric-acid.html acid)(S-20098) Cat. No.: HY-17038 (S-20098 L(+)-Tartaric acid) Cat. No.: HY-17038BAgomelatine (S-20098) is a specific agonist ofMT1 and M

19、T2 receptors with Ks of 0.1, 0.06,i0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1,CHO-hMT2, and HEK-hMT2, respectively.Agomelatine L(+)-Tartaric acid (S-20098L(+)-Tartaric acid) is a specific agonist ofMT1 and MT2 receptors with Ks of 0.1, 0.06,i0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1,CHO-hMT2, and HEK-h

20、MT2, respectively.Purity: 98.77%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.82%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/agomelatine-hydrochloride.html

21、Agomelatine HYPERLINK https:/www.MedChemE/agomelatine-hydrochloride.html HYPERLINK https:/www.MedChemE/agomelatine-hydrochloride.html hydrochloride(S-20098 hydrochloride) Cat. No.: HY-17038A HYPERLINK https:/www.MedChemE/agomelatine-d4.html Agomelatine-d4(S-20098-d4) Cat. No.: HY-17038S1Agomelatine

22、hydrochloride (S-20098 hydrochloride)is a specific agonist of MT1 and MT2receptors with Ks of 0.1, 0.06, 0.12, and 0.27 nMifor CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2,respectively.Agomelatine-d4 (S-20098-d4) is the deuteriumlabeled Agomelatine. Agomelatine (S-20098) is aspecific agonist of MT1 an

23、d MT2 receptorswith Ks of 0.1, 0.06, 0.12, and 0.27 nM foriCHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2,respectively.Purity: 99.55%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/agomela

24、tine-d6.html Agomelatine-d6(S-20098-d6) Cat. No.: HY-17038S HYPERLINK https:/www.MedChemE/dh97.html DH97Cat. No.: HY-107628Agomelatine-d6 (S-20098-d6) is deuterium labeledAgomelatine. Agomelatine is a specific agonist ofMT1 and MT2 receptors .DH97 is a potent and selective antagonist ofMT melatonin

25、receptor2 , with a pKi of 8.03for human MT . DH97 shows 89- and 229-fold2selectivity for human MT over human mt and2 1Xenopus mel receptor subtypes.1cPurity: 98%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK

26、https:/www.MedChemE/luzindole.html Luzindole(N-0774) Cat. No.: HY-101254 HYPERLINK https:/www.MedChemE/Melatonin.html Melatonin(N-Acetyl-5-methoxytryptamine) Cat. No.: HY-B0075Luzindole (N-0774) is a selective melatoninreceptor antagonist. Luzindole preferentiallytargets MT2 (Mel ) over MT1 (Mel ) w

27、ith1b 1a Kivalues of 10.2 and 158 nM for human MT2 and MT1,respectively.Melatonin is a hormone made by the pineal glandthat can activates melatonin receptor.Melatonin plays a role in sleep and possessesimportant antioxidative and anti-inflammatoryproperties.Purity: 100.0%Clinical Data: No Developmen

28、t ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 99.73%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/melatonin-d3.html Melatonin-d3 HYPERLINK https:/www.MedChemE/melatonin-d3.html HYPERLINK https:/www.MedChemE/melatonin-d5.html Melatonin-d4(N-Acetyl-5-me

29、thoxytryptamine-d3) Cat. No.: HY-B0075S1 (N-Acetyl-5-methoxytryptamine-d4) Cat. No.: HY-B0075SMelatonin-d3 (N-Acetyl-5-methoxytryptamine-d3) isthe deuterium labeled Melatonin. Melatonin is ahormone made by the pineal gland that canactivates melatonin receptor.Melatonin D4 is deuterium labeled Melato

30、nin.Melatonin is a hormone made by the pineal glandthat can activates melatonin receptor.Antioxidative and anti-inflammatory properties.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.87%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.Me

31、dChemE/melatonin-d7.html Melatonin-d7 HYPERLINK https:/www.MedChemE/melatonin-d7.html HYPERLINK https:/www.MedChemE/n-acetyltryptamine.html N-Acetyltryptamine HYPERLINK https:/www.MedChemE/n-acetyltryptamine.html (N10-Acetyltryptamine;(N-Acetyl-5-methoxytryptamine-d7) Cat. No.: HY-B0075S2 Nb-Acetylt

32、ryptamine; N-Acetyltryptamine) Cat. No.: HY-100908Melatonin-d7 (N-Acetyl-5-methoxytryptamine-d7) isthe deuterium labeled Melatonin. Melatonin is ahormone made by the pineal gland that canactivates melatonin receptor.N-Acetyltryptamine is a partial agonist formelatonin receptors in the retina.N-Acety

33、ltryptamine is also used for determinationof serotonin N-acetyl transferase activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/piromelatine.html Piromelatine(Ne

34、u-P11) Cat. No.: HY-105285 HYPERLINK https:/www.MedChemE/ramelteon.html Ramelteon(TAK-375) Cat. No.: HY-A0014Piromelatine (Neu-P11) is a melatoninMT1/MT2 receptor agonist, serotonin5-HT1A/5-HT1D agonist, and serotonin 5-HT2Bantagonist.Ramelteon is a potent, highly selective, andorally active agonist

35、 of MT1/MT2 with Ki valuesof 14 and 112 pM, respectively. Ramelteon has thepotential for the research of insomnia.Purity: 99.21%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.87%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg HYPERLINK https:

36、/www.MedChemE/Ramelteon_metabolite_M-II.html Ramelteon HYPERLINK https:/www.MedChemE/Ramelteon_metabolite_M-II.html HYPERLINK https:/www.MedChemE/Ramelteon_metabolite_M-II.html metabolite HYPERLINK https:/www.MedChemE/Ramelteon_metabolite_M-II.html HYPERLINK https:/www.MedChemE/Ramelteon_metabolite_

37、M-II.html M-II HYPERLINK https:/www.MedChemE/Ramelteon_metabolite_M-II.html HYPERLINK https:/www.MedChemE/ramelteon-metabolite-m-ii-d3.html Ramelteon HYPERLINK https:/www.MedChemE/ramelteon-metabolite-m-ii-d3.html HYPERLINK https:/www.MedChemE/ramelteon-metabolite-m-ii-d3.html metabolite HYPERLINK h

38、ttps:/www.MedChemE/ramelteon-metabolite-m-ii-d3.html HYPERLINK https:/www.MedChemE/ramelteon-metabolite-m-ii-d3.html M-II-d3Cat. No.: HY-103005 Cat. No.: HY-103005SRamelteon metabolite M-II is the major metaboliteof Ramelteon, with IC s of 208 pM, 1470 pM for50human melatonin receptors (MT or MT ).1

39、 2Ramelteon is a selective melatonin agonist.Ramelteon metabolite M-II-d3 is the deuteriumlabeled Ramelteon metabolite M-II. Ramelteonmetabolite M-II is the major metabolite ofRamelteon, with IC s of 208 pM, 1470 pM for human50melatonin receptors (MT or MT ). Ramelteon1 2is a selective melatonin ago

40、nist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/ramelteon-d5.html Ramelteon-d5(TAK-375-d5) Cat. No.: HY-A0014S HYPERLINK https:/www.MedChemE/s-22153.html S-22153Cat. No.: HY-114962R

41、amelteon-d5 is deuterium labeled Ramelteon.Ramelteon is a potent, highly selective, andorally active agonist of MT1/MT2 with Ki values of14 and 112 pM, respectively. Ramelteon has thepotential for the research of insomnia.S-22153 is a potent melatonin receptorantagonist with EC values of 19 nM, 4.6

42、nM for50hMT1 and hMT2 melatonin receptor,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/s26131.html S26131 HYPERLINK https:/www.MedChemE/s26131.html H

43、YPERLINK https:/www.MedChemE/Tasimelteon.html TasimelteonCat. No.: HY-122136(BMS-214778; VEC-162) Cat. No.: HY-14803S26131 (compound 5) is a potent and selectiveMT1 melatoninergic ligand, and the K valuesiare 0.5 and 112 nM for MT1 and MT2, respectively.S26131 behaves as an MT1 and MT2 antagonist.Tasimelteon (BMS-214778) is an orally active andselective dual melatonin receptor agonist(DMRA). Tasimelteon has 2.1-4.4 times greateraffinity for the MT2 receptor than f