Neurotensin-Receptor-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Neurotensin HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html ReceptorThe neuropeptide neurotensin (NT) exerts central actionsthat include hypothermia, analg

2、esia, and a number of effects that involvethe modulation of nigrostriatal and mesocortico-limbic dopaminergic pathways. The two neurotensin receptor subtypes known todate, NTR1 and NTR2, belong to the family of G-protein-coupled receptors with seven putative transmembrane domains (TM). TheNTR1 has h

3、igh affinity for neurotensin, whereas the NTR2 has lower affinity for the peptide and is selectively recognized bylevocabastine, an anti-histamine H1 receptor antagonist. These receptors have widespread, though not identical, central andperipheral distributions and exhibit distinct ontogenic profile

4、s.It is notably reported that NTR1 activation results in significant antinociception but also causes marked hypotension andhypothermia. In sharp contrast, NTR2 has emerged as an important pain target because NTR2-selective analogues exhibit potentanalgesic activity in both acute and chronic pain con

5、ditions in dose-dependent analgesic effects without inducing drop in bloodpressure or body temperature.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Neurotensin HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neur

6、otensin Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Inh

7、ibitors, HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Modulators HYPERLINK h

8、ttps:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Neurotensin Receptor.html Activators HYPERLINK https:/www.MedChemE/AF38469.html

9、 AF38469 HYPERLINK https:/www.MedChemE/AF38469.html HYPERLINK https:/www.MedChemE/af40431.html AF40431Cat. No.: HY-12802 Cat. No.: HY-124673AF38469 is a selective, orally bioavailableSortilin inhibitor with an IC value of 330 nM.50AF40431, the first reported small-molecule ligandof sortilin, has an

10、IC of 4.4 M and a of50 Kd0.7 M . AF40431 is bound in theneurotensin-binding site of sortilin.Purity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.17%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK ht

11、tps:/www.MedChemE/jmv-449.html JMV HYPERLINK https:/www.MedChemE/jmv-449.html HYPERLINK https:/www.MedChemE/jmv-449.html 449 HYPERLINK https:/www.MedChemE/jmv-449.html HYPERLINK https:/www.MedChemE/jmv-449-acetate.html JMV HYPERLINK https:/www.MedChemE/jmv-449-acetate.html HYPERLINK https:/www.MedCh

12、emE/jmv-449-acetate.html 449 HYPERLINK https:/www.MedChemE/jmv-449-acetate.html HYPERLINK https:/www.MedChemE/jmv-449-acetate.html acetateCat. No.: HY-P1256 Cat. No.: HY-P1256CJMV 449 is a potent neurotensin receptor agonist.JMV 449 shows an IC of 0.15 nM for inhibition of50125I-neurotensin binding

13、to neonatal mouse brainand an EC of 1.9 nM in contracting the50guinea-pig ileum.JMV 449 acetate is a potent neurotensin receptoragonist. JMV 449 acetate shows an IC of 0.15 nM50for inhibition of 125I-neurotensin binding toneonatal mouse brain and an EC of 1.9 nM in50contracting the guinea-pig ileum.

14、Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/Kinetensin.html Kinetensin(Kinetensin (human) Cat. No.: HY-P1255 HYPERLINK https:/www.MedChemE/levocabastine-hydrochloride.html Levocabastine

15、HYPERLINK https:/www.MedChemE/levocabastine-hydrochloride.html HYPERLINK https:/www.MedChemE/levocabastine-hydrochloride.html hydrochloride(R 50547 hydrochloride) Cat. No.: HY-14277AKinetensin is a neurotensin-like peptide isolatedfrom pepsin-treated human plasma.Levocabastine (R 50547) hydrochlorid

16、e is a longacting, highly potent and selective histamineH1-receptor antagonist with anti-allergicactivity.Purity: 99.21%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.0%Clinical Data: LaunchedSize: 5 mg HYPERLINK https:/www.MedChemE/levocabastine-d4-hydrochloride.html Levoca

17、bastine-d4 HYPERLINK https:/www.MedChemE/levocabastine-d4-hydrochloride.html HYPERLINK https:/www.MedChemE/levocabastine-d4-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/levocabastine-d4-hydrochloride.html HYPERLINK https:/www.MedChemE/meclinertant.html Meclinertant(R 50547-d4 hydro

18、chloride) Cat. No.: HY-14277AS (SR 48692) Cat. No.: HY-105189Levocabastine-d4 (R 50547-d4) hydrochlorideis thedeuterium labeled Levocabastine hydrochloride.Levocabastine (R 50547) hydrochloride is a longacting, highly potent and selective histamineH1-receptor antagonist with anti-allergicactivity.Me

19、clinertant (SR 48692) is a potent, selective,nonpeptide and orally active neurotensin receptor 1(NTS1) antagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.05%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/ML314.html ML314 HYPERLINK https

20、:/www.MedChemE/ML314.html HYPERLINK https:/www.MedChemE/Neurotensin.html NeurotensinCat. No.: HY-16639 Cat. No.: HY-P0234ML314 is a potent molecule agonist of NTR1 (EC50 =1.9 M); showed good selectivity against NTR2 andGPR35, but did not stimulate Ca2+ mobilization.Neurotensin, a gut tridecapeptide,

21、 acts as apotent cellular mitogen for various colorectal andpancreatic cancers which possess high-affinityneurotensin receptors (NTR).Purity: 99.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 97.40%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 1

22、0 mg, 25 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Neurotensin_8-13_.html Neurotensin(8-13) HYPERLINK https:/www.MedChemE/Neurotensin_8-13_.html HYPERLINK https:/www.MedChemE/ntrc-824.html NTRC-824Cat. No.: HY-P0251 Cat. No.: HY-12436Neurotensin (8-13

23、) is an active fragment ofNeurotensin. Neurotensin(8-13) results in adecrease in cell-surface NT1 receptors (NTR1)density.NTRC-824 (Compound 5) is a potent, selective andneurotensin-like nonpeptide neurotensin receptortype 2 (NTS2) antagonist with an IC of 38 nM50and a K of 202 nM. NTRC-824 is 150-f

24、oldiselectivity for NTS2 over NTS1 (K 30 M).iPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/sbi-553.html SBI-553 HYPERLINK https:/www.MedChemE/sbi-553.html HYPERLINK https:/w

25、ww.MedChemE/sort-pgrn-interaction-inhibitor-1.html SORT-PGRN HYPERLINK https:/www.MedChemE/sort-pgrn-interaction-inhibitor-1.html HYPERLINK https:/www.MedChemE/sort-pgrn-interaction-inhibitor-1.html interaction HYPERLINK https:/www.MedChemE/sort-pgrn-interaction-inhibitor-1.html HYPERLINK https:/www

26、.MedChemE/sort-pgrn-interaction-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/sort-pgrn-interaction-inhibitor-1.html HYPERLINK https:/www.MedChemE/sort-pgrn-interaction-inhibitor-1.html 1Cat. No.: HY-125880 Cat. No.: HY-115213SBI-553 is a potent and brain penetrant NTR1allosteric modulato

27、r, with an EC of 0.34 M.50SORT-PGRN interaction inhibitor 1 is a potentinhibitor of the sortilin-progranulin interactionwith an IC of 2 M.50Purity: 98.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.49%Clinical Data: No Development ReportedSize:

28、 100 mg, 250 mg HYPERLINK https:/www.MedChemE/vgd071.html VGD071 HYPERLINK https:/www.MedChemE/vgd071.html HYPERLINK https:/www.MedChemE/zendusortide.html ZendusortideCat. No.: HY-139668 Cat. No.: HY-P3391VGD071, a sortilin-targeting compound, is apromising candidate for future studies using mousebr

29、east cancer models.Zendusortide is a sortilin binding peptide.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/d-trp11-neurotensin.html D-Trp11-Neurotensin HYPERLINK https:/www.MedChemE/d-trp11-neurotensin.html HYPERLINK https:/www.MedCh