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BIM 23127
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIM 23127图片
CAS NO:160161-61-5
包装:1mg
市场价:1439元

产品介绍
Antagonist of neuromedin B receptor
Cas No.160161-61-5
Canonical SMILESCC([C@@]1([H])/C(O)=N/[C@@](/C(O)=N/[C@](C(O)=N)([H])CC2=CC3=CC=CC=C3C=C2)([H])CSSC[C@@](/N=C(O)/[C@@](N)([H])CC4=CC5=CC=CC=C5C=C4)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/1)([H])CCCN)([H])CC6=CNC7=CC=CC=C67)([H])CC8=CC=C(O)C=C8)C
分子式C62H71N11O9S2
分子量1178.43
溶解度Soluble to 2 mg/ml in 20% acetonitrile
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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) [2].

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 [3].

Clinical trial: Up to now, BIM 23127 is still in the preclinical development stage.

Reference:
[1] Ladenheim EE, Taylor JE, Coy DH, Moran TH.  Blockade of feeding inhibition by neuromedin B using a selective receptor antagonist. Eur J Pharmacol. 1994 Dec 12;271(1):R7-9.