BIM 23127

Ki: 20.9 nM for neuromedin B receptors Bombesin (BN) belongs to a family of neuropeptides whose members, as well as their respective receptors, are widely distributed throughout the mammalian central nervous system (CNS). BN and its related peptides modulate behaviors such as spontaneous activities and feeding. BIM 23127 (D-Nal-cyclo[Cys-Tyr-D-Trp-Orn-Val-Cys]-Nal-NH2) is a neuromedin B receptor antagonist. In vitro: BIM 23127 was reported to potenly give antagonist effect on neuromedin B receptor (Ki = 20.9 nM). In addition, BIM 23127 was also found to be a selective neuromedin B receptor antagonist (> 10000 nM for gastrin-releasing peptide receptors) . In vivo: Prior administration of 100 nmol/kg of BIM 23127 completely blocked the glucose intake suppression produced by neuromedin B. BIM 23127 also completely blocked suppression of intake produced by neuromedin B rather than by neuromedin C. These results suggest an independent role for neuromedin B receptors in suppression of food intake by bombesin-like peptides . Clinical trial: Up to now, BIM 23127 is still in the preclinical development stage.

Product information

CAS Number: 160161-61-5

Molecular Weight: 1178.43

Formula: C62H71N11O9S2

Chemical Name: (2R)-2-[(Z)-{[(4R,7S,10S,13S,16S,19R)-19-[(Z)-[(2R)-2-amino-1-hydroxy-3-(naphthalen-2-yl)propylidene]amino]-10-(3-aminopropyl)-6,9,12,15,18-pentahydroxy-16-[(4-hydroxyphenyl)methyl]-13-[(1H-indol-3-yl)methyl]-7-(propan-2-yl)-1,2-dithia-5,8,11,14,17-pentaazacycloicosa-5,8,11,14,17-pentaen-4-yl](hydroxy)methylidene}amino]-3-(naphthalen-2-yl)propanimidic acid

Smiles: CC(C)[C@@H]1N=C(O)[C@H](CCCN)N=C(O)[C@H](CC2=CNC3=CC=CC=C32)N=C(O)[C@H](CC2=CC=C(O)C=C2)N=C(O)[C@H](CSSC[C@H](N=C1O)/C(/O)=N/[C@H](CC1C=CC2=CC=CC=C2C=1)C(=N)O)/N=C(\O)/[C@H](N)CC1C=CC2=CC=CC=C2C=1 |c:4,12,28,41,t:50|

InChiKey: GLVLDCUADDSQSK-CCNIVULGSA-N

InChi: InChI=1S/C62H71N11O9S2/c1-35(2)54-62(82)72-53(60(80)68-49(55(65)75)30-38-18-22-40-11-4-6-13-42(40)27-38)34-84-83-33-52(71-56(76)46(64)28-37-17-21-39-10-3-5-12-41(39)26-37)61(81)69-50(29-36-19-23-44(74)24-20-36)58(78)70-51(31-43-32-66-47-15-8-7-14-45(43)47)59(79)67-48(16-9-25-63)57(77)73-54/h3-8,10-15,17-24,26-27,32,35,46,48-54,66,74H,9,16,25,28-31,33-34,63-64H2,1-2H3,(H2,65,75)(H,67,79)(H,68,80)(H,69,81)(H,70,78)(H,71,76)(H,72,82)(H,73,77)/t46-,48+,49-,50+,51+,52+,53+,54+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.