Opioid-Receptor-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Opioid HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html ReceptorOpioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids

2、 are dynorphins,enkephalins, endorphins, endomorphins and nociceptin. Opioid receptors are distributed widely in the brain, and are found in thespinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances.Opioid receptors inhibit

3、the transmission of impulse in excitatory pathways within the human body system. These pathways includethe serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being.Opioid receptors are further subclassified into mu, delta, and kappa r

4、eceptors. All the classes, while exhibiting differing modes ofaction, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasmamembrane of the majority of cells.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Opioid HYP

5、ERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Opioid Rec

6、eptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChem

7、E/Targets/Opioid Receptor.html Modulators HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Opioid Receptor.html Activators HYPERLINK

8、 https:/www.MedChemE/racemic-j-113397.html ()-J-113397 HYPERLINK https:/www.MedChemE/racemic-j-113397.html HYPERLINK https:/www.MedChemE/6-gnti-dihydrochloride.html 6-GNTI HYPERLINK https:/www.MedChemE/6-gnti-dihydrochloride.html HYPERLINK https:/www.MedChemE/6-gnti-dihydrochloride.html dihydrochlor

9、ideCat. No.: HY-107721 Cat. No.: HY-110302()-J-113397 is a potent and selectivenon-peptidyl ORL1 receptor antagonist with a Kof 1.8 nM for cloned human ORL1. J-113397iinhibited nociceptin/orphanin FQ-stimulated GTPSbinding to CHO cells expressing ORL1 with an IC50value of 5.3 nM.6-GNTI dihydrochlori

10、de, a -opioid receptor (KOR)agonist, displays bias toward the activation of Gprotein-mediated signaling over -arrestin2recruitment. 6-GNTI 6-GNTI dihydrochloride onlyactivates the Akt pathway in striatal neurons.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Dat

11、a: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/6-Alpha-Naloxol.html 6-Alpha HYPERLINK https:/www.MedChemE/6-Alpha-Naloxol.html HYPERLINK https:/www.MedChemE/6-Alpha-Naloxol.html Naloxol(Alpha-Naloxol) Cat. No.: HY-12799 HYPERLINK https:/www.MedChemE/6-beta-Naloxol-D5-hydroc

12、hloride.html 6-beta-Naloxol HYPERLINK https:/www.MedChemE/6-beta-Naloxol-D5-hydrochloride.html HYPERLINK https:/www.MedChemE/6-beta-Naloxol-D5-hydrochloride.html D5 HYPERLINK https:/www.MedChemE/6-beta-Naloxol-D5-hydrochloride.html HYPERLINK https:/www.MedChemE/6-beta-Naloxol-D5-hydrochloride.html h

13、ydrochloride(6-Naloxol D5 hydrochloride) Cat. No.: HY-12780S6-Alpha Naloxol(Alpha-Naloxol) is an opioidantagonist closely related to naloxone; a humanmetabolite of naloxone.6-beta-Naloxol D5 hydrochloride is the deuteriumlabeled 6-beta-Naloxol, which is an opioidantagonist closely related to naloxon

14、e.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/ac-ryyrik-nh2.html Ac-RYYRIK-NH2 HYPERLINK https:/www.MedChemE/ac-ryyrik-nh2.html HYPERLINK https:/www.MedChemE/ac-ryyrik-nh2-tfa.html Ac

15、-RYYRIK-NH2 HYPERLINK https:/www.MedChemE/ac-ryyrik-nh2-tfa.html HYPERLINK https:/www.MedChemE/ac-ryyrik-nh2-tfa.html TFACat. No.: HY-P1318 Cat. No.: HY-P1318AAc-RYYRIK-NH2 is a potent and partial agonist onORL1 transfected in CHO cells (K =1.5 nM) anddbehaves as a endogenous ligand of ORL1.Ac-RYYRI

16、K-NH2 TFA is a potent and partial agoniston ORL1 transfected in CHO cells (K =1.5 nM)dand behaves as a endogenous ligand of ORL1.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/ac-ryyrwk-

17、nh2.html Ac-RYYRWK-NH2 HYPERLINK https:/www.MedChemE/ac-ryyrwk-nh2.html HYPERLINK https:/www.MedChemE/ac-ryyrwk-nh2-tfa.html Ac-RYYRWK-NH2 HYPERLINK https:/www.MedChemE/ac-ryyrwk-nh2-tfa.html HYPERLINK https:/www.MedChemE/ac-ryyrwk-nh2-tfa.html TFACat. No.: HY-P1316 Cat. No.: HY-P1316AAc-RYYRWK-NH2

18、is a potent and selective partialagonist for the nociceptin receptor (NOP),3HAc-RYYRWK-NH2 binds to rat corticalmembranes ORL1 with a K of 0.071 nM, but has nodaffinity for -, - or -opioid receptors.Ac-RYYRWK-NH2 is a potent and selective partialagonist for the nociceptin receptor (NOP),3HAc-RYYRWK-

19、NH2 binds to rat corticalmembranes ORL1 with a K of 0.071 nM, but has nodaffinity for -, - or -opioid receptors.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/acetyl-tetrapeptide-15.html

20、 Acetyl HYPERLINK https:/www.MedChemE/acetyl-tetrapeptide-15.html HYPERLINK https:/www.MedChemE/acetyl-tetrapeptide-15.html tetrapeptide-15 HYPERLINK https:/www.MedChemE/acetyl-tetrapeptide-15.html HYPERLINK https:/www.MedChemE/ADL-5859.html ADL-5859Cat. No.: HY-P1626 Cat. No.: HY-13044Acetyl tetrap

21、eptide-15 is a synthetic peptide usedin the cosmetics for sensitive skin. Acetyltetrapeptide-15 is derived from endomorphin-2(Tyr-Pro-Phe-Phe-NH2), a human -opioid agonistwith selective anti-nociceptive effect.ADL5859 is a -opioid receptor agonist with Ki of0.8 nM, selectivity against opioid recepto

22、r , ,and weak inhibitory activity at the hERG channel.Purity: 98%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.77%Clinical Data: Phase 2Size: 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.MedC

23、hemE/Adrenorphin.html Adrenorphin(Metorphamide) Cat. No.: HY-P1087 HYPERLINK https:/www.MedChemE/akuammidine.html AkuammidineCat. No.: HY-N7437Adrenorphin is a opioid octapeptide, acting as apotent agonist of -opioid receptor, with K of 12inM.Akuammidine, isolated from the seeds ofPicralima nitida,

24、shows a preference for -opioidbinding sites with K values of 0.6, 2.4 and 8.6iM at -, - and -opioid binding sites,respectively. Akuammidine possessesanti-inflammatory and anti-asthmatic properties.Purity: 95.49%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Develo

25、pment ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/alvimopan.html Alvimopan(ADL 8-2698; LY 246736) Cat. No.: HY-13243 HYPERLINK https:/www.MedChemE/alvimopan-dihydrate.html Alvimopan HYPERLINK https:/www.MedChemE/alvimopan-dihydrate.html HYPERLINK https:/www.MedChemE/alvimopan-dihy

26、drate.html dihydrate(ADL 8-2698 dihydrate; LY 246736 dihydrate) Cat. No.: HY-76657AAlvimopan (ADL 8-2698) is a potent, selective,orally active and reversible -opioid receptorantagonist, with an IC of 1.7 nM. Alvimopan has50selectivity for -opioid receptor (K=0.47 nM)iover - and -opioid receptors (Ks

27、=100, 12 nM,irespectively).Alvimopan dihydrate (ADL 8-2698 dihydrate) is apotent, selective, orally active and reversible-opioid receptor antagonist, with an IC of 1.750nM.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98.70%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPE

28、RLINK https:/www.MedChemE/alvimopan-monohydrate.html Alvimopan HYPERLINK https:/www.MedChemE/alvimopan-monohydrate.html HYPERLINK https:/www.MedChemE/alvimopan-monohydrate.html monohydrate(ADL 8-2698 monohydrate; LY 246736 monohydrate) Cat. No.: HY-76657 HYPERLINK https:/www.MedChemE/alvimopan-d5.ht

29、ml Alvimopan-d5Cat. No.: HY-13243SAlvimopan monohydrate (ADL 8-2698 monohydrate) isa potent, selective, orally active and reversible-opioid receptor antagonist, with an IC of 1.750nM.Alvimopan-d5 is the deuterium labeled Alvimopan.Alvimopan (ADL 8-2698) is a potent, selective,orally active and rever

30、sible -opioid receptorantagonist, with an IC of 1.7 nM.50Purity: 99.18%Clinical Data: LaunchedSize: 2 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/AR-M_1000390_hydrochloride.html AR-M HYPERLINK https:/www.MedChemE/AR-M_1000390_hydrochloride.html

31、HYPERLINK https:/www.MedChemE/AR-M_1000390_hydrochloride.html 1000390 HYPERLINK https:/www.MedChemE/AR-M_1000390_hydrochloride.html HYPERLINK https:/www.MedChemE/AR-M_1000390_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/AR-M_1000390_hydrochloride.html HYPERLINK https:/www.MedChemE/

32、Asimadoline.html AsimadolineCat. No.: HY-101039A(EMD-61753) Cat. No.: HY-107384AR-M 1000390 hydrochloride is an exceptionallyselective, potent opioid receptor agonist withan EC of 7.20.9 nM for agonist potency.50Asimadoline (EMD-61753) is an orally active,selective and peripherally active -opioid ag

33、onistwith IC s of 5.6 nM (guinea pig) and 1.2 nM50(human recombinant).Purity: 99.56%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.36%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/asimadoline-hydrochloride.html

34、Asimadoline HYPERLINK https:/www.MedChemE/asimadoline-hydrochloride.html HYPERLINK https:/www.MedChemE/asimadoline-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/asimadoline-hydrochloride.html HYPERLINK https:/www.MedChemE/asimadoline-d3-hydrochloride.html Asimadoline-d5 HYPERLINK ht

35、tps:/www.MedChemE/asimadoline-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/asimadoline-d3-hydrochloride.html hydrochloride(EMD-61753 hydrochloride) Cat. No.: HY-107384ACat. No.: HY-107384ASAsimadoline (EMD-61753) hydrochloride is an orallyactive, selective and peripherally active -opioidagoni

36、st with IC s of 5.6 nM (guinea pig) and 1.250nM (human recombinant).Asimadoline-d5 hydrochloride is the deuteriumlabeled Asimadoline hydrochloride. Asimadoline(EMD-61753) hydrochloride is an orally active,selective and peripherally active -opioid agonistwith IC s of 5.6 nM (guinea pig) and 1.2 nM50(

37、human recombinant).Purity: 99.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/at-121.html AT-121 HYPERLINK https:/www.MedChemE/at-121.html HYPERLINK https:/www.M

38、edChemE/at-121-hydrochloride.html AT-121 HYPERLINK https:/www.MedChemE/at-121-hydrochloride.html HYPERLINK https:/www.MedChemE/at-121-hydrochloride.html hydrochlorideCat. No.: HY-112692 Cat. No.: HY-112692AAT-121 is a bifunctional nociception and muopioid receptor agonist, with Ks of 3.67 andi16.49

39、nM, respectively. AT-121 is a safe,non-addictive analgesic, and shows antinociceptiveand antiallodynic effects.AT-121 hydrochloride is a bifunctional nociceptionand mu opioid receptor agonist, with Ks ofi3.67 and 16.49 nM, respectively. AT-121hydrochloride is a safe, non-addictive analgesic,and show

40、s antinociceptive and antiallodyniceffects.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/LY-2456302.html Aticaprant(CERC-501; LY-2456302) Cat. No.: HY-101718 HYPERLINK https:/www.MedChe

41、mE/BAM-22P.html BAM-22P(Bovine adrenal medulla-22P) Cat. No.: HY-P1331Aticaprant (CERC-501) is a potent andcentrally-penetrant kappa opioid receptorantagonist with a K of 0.807 nM.iBAM-22P, a highly potent opioid peptide, is apotent opioid agonist.Purity: 99.86%Clinical Data: Phase 2Size: 10 mM 1 mL

42、, 1 mg, 5 mg, 10 mg, 20 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 500 g, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/BAN-ORL-24.html BAN HYPERLINK https:/www.MedChemE/BAN-ORL-24.html HYPERLINK https:/www.MedChemE/BAN-ORL-24.html ORL HYPERLINK https:/www.MedChemE/BAN-ORL-24.html HY

43、PERLINK https:/www.MedChemE/BAN-ORL-24.html 24Cat. No.: HY-13222 HYPERLINK https:/www.MedChemE/Bevenopran.html Bevenopran(CB-5945; ADL-5945) Cat. No.: HY-100122BAN ORL 24 is a potent and selective NOP receptorantagonist. (IC50 values are 0.27, 2500, 6700 and 10000 nM for NOP, -, - and -receptorsresp

44、ectively).Bevenopran is a peripheral -opioid receptorantagonist.Purity: 98.09%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 3Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Bisacodyl.html Bisacodyl HYPERLINK https:/www.MedChemE/Bisacodyl.h

45、tml HYPERLINK https:/www.MedChemE/bms-986121.html BMS-986121Cat. No.: HY-B0557 Cat. No.: HY-141515Bisacodyl is a stimulant laxative agent that worksdirectly on the colon to produce a bowel movement.Bisacodyl increases the secretion of PGE by2direct activation of colon macrophages.BMS-986121 is a pos

46、itive allosteric modulator(PAM) of the opioid receptor extracted frompatent WO2014107344. BMS-986121 is built on achemical scaffold representing a new chemotype for receptor PAMs.Purity: 99.18%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 5 gPurity: 98%Clinical Data: No Development ReportedSize:

47、1 mg, 5 mg HYPERLINK https:/www.MedChemE/bms-986122.html BMS-986122 HYPERLINK https:/www.MedChemE/bms-986122.html HYPERLINK https:/www.MedChemE/bms-986187.html BMS-986187Cat. No.: HY-120645 Cat. No.: HY-120613BMS-986122 is a selective, potent positiveallosteric modulator of the mu-opioid receptor(-O

48、R). BMS-986122 shows potentiation oforthosteric agonist-mediated -arrestinrecruitment, adenylyl cyclase inhibition, and Gprotein activation.BMS-986187 is an -opioid receptor-selectivepositive allosteric modulator (PAM) with an EC50of 0.03 M and a pK of 6.02 (1 M).BBMS-986187 has no observable PAM ac

49、tivity atthe -receptor (EC =3 M).50Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/bms-986188.html B

50、MS-986188 HYPERLINK https:/www.MedChemE/bms-986188.html HYPERLINK https:/www.MedChemE/bpr1m97.html BPR1M97Cat. No.: HY-120024 Cat. No.: HY-128865BMS-986188 is a selective positive allostericmodulator of -opioid receptor with an EC of500.05 M.BPR1M97 is a dual-acting mu opioid receptor(MOP) and nocic

51、eptin-orphanin FQ peptide (NOP)receptor agonist with K values of 1.8 and 4.2inM, respectively. BPR1M97 shows high potency andblood-brain barrier penetration, and producespotent antinociceptive effects.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.99%Clinical Data: No De

52、velopment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/btrx-335140.html BTRX-335140(CYM-53093) Cat. No.: HY-124754 HYPERLINK https:/www.MedChemE/bw373u86.html BW373U86(SNC86) Cat. No.: HY-107751BTRX-335140 (CYM-53093) is a potent and selective,orally acti

53、ve opioid receptor (KOR)antagonist, has antagonist activity for OR, ORand OR with IC values of 0.8 nM, 110 nM, and506500 nM, respectively.BW373U86 (SNC86) is a -opioid receptor agonistwith an IC of 1.49 nM. BW373U86 shows50antidepressant-like effects.Purity: 99.71%Clinical Data: Phase 2Size: 10 mM 1

54、 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ccg258747.html CCG258747Cat. No.: HY-139690 HYPERLINK https:/www.MedChemE/cebranopadol.html Cebranopadol(GRT6005) Cat. No.: HY-15536CCG258747 is a selective GRK2 inhibitor (IC =1850

55、nM) with high selectivity over GRK1, GRK5, PKA,and ROCK1 (518, 83, 5500, and 550fold,respectively).CCG258747 also blocks theinternalization of the -opioid receptor.Cebranopadol is an analgesic NOP and opioidreceptor agonist with Ks/ s of 0.9 nM/13i EC50nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM f

56、orhuman NOP, MOP, KOP and delta-opioid peptide (DOP)receptor, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 96.91%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Cebranopadol-_1_alpha_,4_alpha_stereoisomer.html Cebranop

57、adol HYPERLINK https:/www.MedChemE/Cebranopadol-_1_alpha_,4_alpha_stereoisomer.html HYPERLINK https:/www.MedChemE/Cebranopadol-_1_alpha_,4_alpha_stereoisomer.html (1,4)stereoisomer) HYPERLINK https:/www.MedChemE/Cebranopadol-_1_alpha_,4_alpha_stereoisomer.html HYPERLINK https:/www.MedChemE/cebranopa

58、dol-d5.html Cebranopadol-d5(GRT6005 (1,4)stereoisomer) Cat. No.: HY-15536A (GRT6005-d5) Cat. No.: HY-15536SCebranopadol (1,4)stereoisomer) is astereoisomer of cebranopadol. Cebranopadol is apotent agonist activity on ORL-1.Cebranopadol-d5 (GRT6005-d5) is the deuteriumlabeled Cebranopadol. Cebranopad

59、ol is an analgesicNOP opioid receptor Ki EC50and agonist with s/ sof 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18nM/110 nM for human NOP, MOP, KOP and delta-opioidpeptide (DOP) receptor, respectively.Purity: 95.59%Clinical Data: No Development ReportedSize: 2 mg, 5 mgPurity: 98%Clinical Data: No De

60、velopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Corydaline.html Corydaline HYPERLINK https:/www.MedChemE/Corydaline.html HYPERLINK https:/www.MedChemE/ctap.html CTAP(+)-Corydaline; Corydalin) Cat. No.: HY-N0923Cat. No.: HY-P1335Corydaline (+)-Corydaline), an isoquinolinealkaloid iso