Melanocortin-Receptor-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html Melanocortin HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html ReceptorMC ReceptorThe melanocortin (MC) receptors represent a subfamily of G-protein-coupl

2、ed receptors (GPCRs) where the different subtypes areinvolved in a wide range of physiological functions such as pigmentation, steroid secretion, energy homeostasis, and food intake.The melanocortin receptor (MCR) family consists of five G-protein-coupled receptors (MC1R-MC5R). MC1R controls pigment

3、ation,MC2R is a critical component of the hypothalamic-pituitary-adrenal axis, MC3R and MC4R have a vital role in energy homeostasisand MC5R is involved in exocrine function.MCRs are activated by a variety of neuropeptides, termed melanocortins, that include the adrenocorticotropic hormone (ACTH)and

4、, and -melanocyte-stimulating hormones (MSHs). Melanocortins derive from post-translational processing of the commonpolypeptide precursor pro-opiomelanocortin, expressed mainly in the hypothalamus and pituitary.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html Melanocor

5、tin HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html Inhibitors, HYPERLINK https

6、:/www.MedChemE/Targets/Melanocortin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html Agonists HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Melano

7、cortin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Melanocortin Receptor.html Antagonists HYPERLINK https:/www.MedChemE/ACTH_1-17.html ACTH HYPERLINK https:/www.MedChemE/ACTH_1-17.html HYPERLINK https:/www.MedChemE/ACTH_1-17.html (1-17)(1-17-ACTH) Cat. No.: HY-P1545 HYPERLINK https:/www.MedC

8、hemE/acth-1-17-tfa.html ACTH HYPERLINK https:/www.MedChemE/acth-1-17-tfa.html HYPERLINK https:/www.MedChemE/acth-1-17-tfa.html (1-17) HYPERLINK https:/www.MedChemE/acth-1-17-tfa.html HYPERLINK https:/www.MedChemE/acth-1-17-tfa.html (TFA)(1-17-ACTH TFA) Cat. No.: HY-P1545AACTH (1-17), an adrenocortic

9、otropin analogue, is apotent human melanocortin 1 (MC1) receptoragonist with a K of 0.21 nM.iACTH (1-17) TFA, an adrenocorticotropin analogue,is a potent human melanocortin 1 (MC1)receptor agonist with a K of 0.21 nM.iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98

10、%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/ACTH_11-24.html ACTH HYPERLINK https:/www.MedChemE/ACTH_11-24.html HYPERLINK https:/www.MedChemE/ACTH_11-24.html (11-24)(Adrenocorticotropic Hormone (11-24) Cat. No.: HY-P1558 HYPERLINK https:/www.MedChemE/A

11、drenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html Adrenocorticotropic HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html Hormone HYPERLINK https:/www.MedChemE/Adrenocorticotr

12、opic_Hormone_ACTH_1-39_,_human_TFA_.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html (ACTH) HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_

13、.html (1-39), HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_human_TFA_.html human(TFA)(1-39-Corticotropin (human)(TFA) Cat. No.: HY-P1211AACTH (11-24) is a fragment ofadrenocorticotrophin, a

14、cts as an antagonist ofadrenocorticotropic hormone (ACTH) receptor, andinduces cortisol release.Adrenocorticotropic Hormone (ACTH) (1-39),human(TFA) is a melanocortin receptor agonist.Purity: 95.40%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.28%Clinical Data: No Developme

15、nt ReportedSize: 500 g, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html Adrenocorticotropic HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html Hormone

16、HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html (ACTH) HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormon

17、e_ACTH_1-39_,_rat.html (1-39), HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat.html rat(ACTH (1-39) (mouse, rat) Cat. No.: HY-P1477 HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_

18、1-39_,_rat_TFA.html Adrenocorticotropic HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html Hormone HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html HYP

19、ERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html (ACTH) HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html (1-39), HYPERLINK https:/www.MedChemE/Adrenocor

20、ticotropic_Hormone_ACTH_1-39_,_rat_TFA.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html rat HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_1-39_,_rat_TFA.html TFA

21、(ACTH (1-39) (mouse, rat) TFA) Cat. No.: HY-P1477AAdrenocorticotropic Hormone (ACTH) (1-39), rat isa potent melanocortin 2 (MC2) receptoragonist.Adrenocorticotropic Hormone (ACTH) (1-39), rat(TFA) is a potent melanocortin 2 (MC2)receptor agonist.Purity: 98%Clinical Data: No Development ReportedSize:

22、 1 mg, 5 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 500 g, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html Adrenocorticotropic HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html HYPERLINK https:/www.MedChemE/A

23、drenocorticotropic_Hormone_ACTH_4-10_,_human.html Hormone HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html (ACTH) HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_hum

24、an.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html (4-10), HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html HYPERLINK https:/www.MedChemE/Adrenocorticotropic_Hormone_ACTH_4-10_,_human.html human HYPERLINK https:/www.MedChemE/Adren

25、ocorticotropic_Hormone_ACTH_4-10_,_human.html HYPERLINK https:/www.MedChemE/bms-470539-dihydrochloride.html BMS-470539 HYPERLINK https:/www.MedChemE/bms-470539-dihydrochloride.html HYPERLINK https:/www.MedChemE/bms-470539-dihydrochloride.html dihydrochlorideCat. No.: HY-P1478 Cat. No.: HY-115644Adre

26、nocorticotropic Hormone (ACTH) (4-10), humanis a melanocortin 4 (MC4R) receptor agonist.BMS-470539 dihydrochloride is a highly potent andselective melanocortin-1 receptor (MC-1R)agonist with an IC of 120 nM, an of 2850 EC50nM. BMS-470539 dihydrochloride does not activateMC-3R and is a very weak part

27、ial agonist at MC-4Rand MC-5R.Purity: 99.49%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98.50%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Bremelanotide-Acetate.html Bremelanotide HYPERLINK https:/www.MedChemE/B

28、remelanotide-Acetate.html HYPERLINK https:/www.MedChemE/Bremelanotide-Acetate.html Acetate HYPERLINK https:/www.MedChemE/Bremelanotide-Acetate.html HYPERLINK https:/www.MedChemE/ccz01048.html CCZ01048(PT-141 Acetate) Cat. No.: HY-18678ACat. No.: HY-P2336Bremelanotide Acetate (PT-141 Acetate), asynth

29、etic peptide analogue of -MSH, is an agonistat melanocortin receptors including the MC3Rand MC4R for the treatment of sexual dysfunction.CCZ01048, a -melanocyte-stimulating hormone(-MSH) analogue, exhibits high binding affinityto melanocortin 1 receptor (MC1R) with a K ofi0.31 nM. CCZ01048 shows rap

30、id internalization intoB16F10 melanoma cells and high in vivo stability.Purity: 99.97%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/ccz0104

31、8-tfa.html CCZ01048 HYPERLINK https:/www.MedChemE/ccz01048-tfa.html HYPERLINK https:/www.MedChemE/ccz01048-tfa.html TFACat. No.: HY-P2336A HYPERLINK https:/www.MedChemE/dersimelagon.html Dersimelagon(MT-7117) Cat. No.: HY-109114CCZ01048 TFA, a -MSH analogue, exhibits highbinding affinity to melanoco

32、rtin 1 receptor(MC1R) with a K of 0.31 nM. CCZ01048 TFA showsirapid internalization into B16F10 melanoma cellsand high in vivo stability.Dersimelagon (MT-7117) is an orally active,selective melanocortin 1 receptor (MC1R)agonist with EC values of 8.16, 3.91, 1.14 and500.251 nM for human (h), cynomolg

33、us monkey (cm),mouse (m) and rat (r) MC1R, respectively.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/fenoprofen.html Fenoprofen(LILLY-53858) Cat. No.: HY-B1456A HYPERLINK https:/www.Me

34、dChemE/hmc1r-agonist-1.html hMC1R HYPERLINK https:/www.MedChemE/hmc1r-agonist-1.html HYPERLINK https:/www.MedChemE/hmc1r-agonist-1.html agonist HYPERLINK https:/www.MedChemE/hmc1r-agonist-1.html HYPERLINK https:/www.MedChemE/hmc1r-agonist-1.html 1Cat. No.: HY-P99004Fenoprofen (LILLY-53858) is a nons

35、teroidalanti-inflammatory agent (NSAID). Fenoprofen can beused to to relieve symptoms of arthritis(osteoarthritis and rheumatoid arthritis), such asinflammation, swelling, stiffness, and joint pain.(EC =3 nM). hMC1R agonist 1 shows at least50300-fold selectivity for hMC1R over hMC3R(bEC =902 nM), (b

36、EC =915 nM),50 hMC4R 50and hMC5R (bEC =1000 nM). hMC1R50agonist 1 has the potential for the therapeuticintervention of melanocortin family.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/

37、hs014.html HS014 HYPERLINK https:/www.MedChemE/hs014.html HYPERLINK https:/www.MedChemE/hs014-tfa.html HS014 HYPERLINK https:/www.MedChemE/hs014-tfa.html HYPERLINK https:/www.MedChemE/hs014-tfa.html TFACat. No.: HY-P1216 Cat. No.: HY-P1216AHS014 is a potent and selective melanocortin-4(MC4) receptor

38、 antagonist, with Ks of 3.16, 108,i54.4 and 694 nM for human MC4, MC1, MC3 and MC5receptors, respectively. HS014 modulates thebehavioral effects of morphine in mice. HS014increases food intake in free-feeding rats.HS014 TFA is a potent and selectivemelanocortin-4 (MC4) receptor antagonist, withKs of

39、 3.16, 108, 54.4 and 694 nM for human MC4,iMC1, MC3 and MC5 receptors respectively. HS014 TFAmodulates the behavioral effects of morphine inmice.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.81%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.

40、MedChemE/hs024.html HS024 HYPERLINK https:/www.MedChemE/hs024.html HYPERLINK https:/www.MedChemE/hs024-tfa.html HS024 HYPERLINK https:/www.MedChemE/hs024-tfa.html HYPERLINK https:/www.MedChemE/hs024-tfa.html TFACat. No.: HY-P1215 Cat. No.: HY-P1215AHS024 is a selective MC4 receptor antagonist,with K

41、s of 0.29, 3.29, 5.45, and 18.6 nM for MC4,iMC5, MC3, and MC1, respectively. HS024 increasefood intake.HS024 is a selective MC4 receptor antagonist,with Ks of 0.29, 3.29, 5.45, 18.6 nM for MC4,iMC5, MC3, and MC1, respectively. HS024 increasefood intake.Purity: 98%Clinical Data: No Development Report

42、edSize: 5 mg, 10 mgPurity: 99.63%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/jkc363.html JKC363 HYPERLINK https:/www.MedChemE/jkc363.html HYPERLINK https:/www.MedChemE/jkc363-tfa.html JKC363 HYPERLINK https:/www.MedChemE/jkc363-tfa.html HYPERLINK https

43、:/www.MedChemE/jkc363-tfa.html TFACat. No.: HY-P1213 Cat. No.: HY-P1213AJKC363, a selective melanocortin MC4 receptorantagonist, has a 90-fold higher affinity at theMC4 receptor (IC =0.5 nM) than at the MC350receptor (44.9 nM). JKC-363 blocks the stimulatoryeffect of -MSH on TRH release. Anti-hypera

44、lgesiceffect.JKC363 TFA, a selective melanocortin MC4receptor antagonist, has a 90-fold higheraffinity at the MC4 receptor (IC =0.5 nM) than at50the MC3 receptor (44.9 nM). JKC363 TFA blocks thestimulatory effect of -MSH on TRH release.Anti-hyperalgesic effect.Purity: 98%Clinical Data: No Developmen

45、t ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/JNJ-10229570.html JNJ-10229570 HYPERLINK https:/www.MedChemE/JNJ-10229570.html HYPERLINK https:/www.MedChemE/lys-3-msh-human.html Lys-3-MSH(human)Cat. No.: HY-10713

46、9 Cat. No.: HY-P1210JNJ-10229570 is an antagonist of melanocortinreceptor 1 (MC1R) and melanocortin receptor5 (MC5R), which inhibits sebaceous glanddifferentiation and the production ofsebum-specific lipids.Lys-3-MSH(human) is a melanocortin peptidederived from the C-terminal of the fragment ofpro-o

47、piomelanocortin (POMC). Lys-3-MSH(human)potentiates the steroidogenic response of the ratadrenal to adrenocorticotrophin (ACTH).Purity: 98.0%Clinical Data: Phase 1Size: 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

48、.MedChemE/Acetamide,_N-1-5-chloro-2-1-_3S,4R_-4-_2,4-difluorophenyl_-1-_1,1-dimethylethyl_-3-pyrrolidinylcarbonyl-4-piperidinylphenylethyl-.html MC-4R HYPERLINK https:/www.MedChemE/Acetamide,_N-1-5-chloro-2-1-_3S,4R_-4-_2,4-difluorophenyl_-1-_1,1-dimethylethyl_-3-pyrrolidinylcarbonyl-4-piperidinylph

49、enylethyl-.html HYPERLINK https:/www.MedChemE/Acetamide,_N-1-5-chloro-2-1-_3S,4R_-4-_2,4-difluorophenyl_-1-_1,1-dimethylethyl_-3-pyrrolidinylcarbonyl-4-piperidinylphenylethyl-.html Agonist HYPERLINK https:/www.MedChemE/Acetamide,_N-1-5-chloro-2-1-_3S,4R_-4-_2,4-difluorophenyl_-1-_1,1-dimethylethyl_-

50、3-pyrrolidinylcarbonyl-4-piperidinylphenylethyl-.html HYPERLINK https:/www.MedChemE/Acetamide,_N-1-5-chloro-2-1-_3S,4R_-4-_2,4-difluorophenyl_-1-_1,1-dimethylethyl_-3-pyrrolidinylcarbonyl-4-piperidinylphenylethyl-.html 1 HYPERLINK https:/www.MedChemE/Acetamide,_N-1-5-chloro-2-1-_3S,4R_-4-_2,4-difluo

51、rophenyl_-1-_1,1-dimethylethyl_-3-pyrrolidinylcarbonyl-4-piperidinylphenylethyl-.html HYPERLINK https:/www.MedChemE/mcl0020.html MCL0020Cat. No.: HY-U00396 Cat. No.: HY-107627MC-4R Agonist 1 is an agonist of humanmelanocortin-4 receptor (MC-4R), used in theresearch of obesity, diabetes, and sexualdy

52、sfunction.MCL0020 is a potent and selective melanocortinMC4 receptor antagonist, with an IC of 11.6350nM. MCL0020 dose-dependently and significantlyattenuates restraint stress-induced anorexiawithout affecting food intake.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Cl

53、inical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mk-0493.html MK-0493 HYPERLINK https:/www.MedChemE/mk-0493.html HYPERLINK https:/www.MedChemE/ml-00253764-hydrochloride.html ML-00253764 HYPERLINK https:/www.MedChemE/ml-00253764-hydrochloride.html HYPERLINK https:/ww

54、w.MedChemE/ml-00253764-hydrochloride.html hydrochlorideCat. No.: HY-118930 Cat. No.: HY-110123MK-0493 is a potent, orally active and selectiveagonist of the melanocortin receptor 4(MC4R), demonstrating significant reductions inenergy intake.ML-00253764 hydrochloride is a brain penetrantnonpeptidic m

55、elanocortin receptor 4 (MC4R)antagonist with a Ki and IC50 of 0.16 M and 0.103M, respectively.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/msg606.html MSG606 HYPERLINK https:/www.MedCh

56、emE/msg606.html HYPERLINK https:/www.MedChemE/msg606-tfa.html MSG606 HYPERLINK https:/www.MedChemE/msg606-tfa.html HYPERLINK https:/www.MedChemE/msg606-tfa.html TFACat. No.: HY-P1726 Cat. No.: HY-P1726AMSG606 is a selective MC1R (melanocortin 1receptor) antagonist and can be used for theresearch of

57、neuroprotective effects.MSG606 TFA is a potent human MC1 receptorantagonist (IC =17 nM). MSG606 TFA also partial50agonist at human MC3 and MC5 receptors (EC50values are 59 and 1300 nM, respectively). MSG606TFA exhibits binding affinity for A375 melanomacells in vitro.Purity: 98%Clinical Data: No Dev

58、elopment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/neuropeptide-ei-rat.html Neuropeptide HYPERLINK https:/www.MedChemE/neuropeptide-ei-rat.html HYPERLINK https:/www.MedChemE/neuropeptide-ei-rat.html EI, HYPERLINK https:/ww

59、w.MedChemE/neuropeptide-ei-rat.html HYPERLINK https:/www.MedChemE/neuropeptide-ei-rat.html rat HYPERLINK https:/www.MedChemE/neuropeptide-ei-rat.html HYPERLINK https:/www.MedChemE/Nonapeptide-1_acetate_salt.html Nonapeptide-1 HYPERLINK https:/www.MedChemE/Nonapeptide-1_acetate_salt.html HYPERLINK ht

60、tps:/www.MedChemE/Nonapeptide-1_acetate_salt.html acetate HYPERLINK https:/www.MedChemE/Nonapeptide-1_acetate_salt.html HYPERLINK https:/www.MedChemE/Nonapeptide-1_acetate_salt.html saltCat. No.: HY-P1869(Melanostatine-5 acetate salt) Cat. No.: HY-P0097ANeuropeptide EI, rat displays functional melan