BIM 189
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:大鼠胰腺的IC50为10.4 nM,豚鼠胰腺的IC50为2.4 nM.
蛙皮素(Bombesin)对胃肠道和摄食行为具有作用.蛙皮素作用于两种受体,包括与神经介素B具有高亲和力的受体以及与蛙皮素和胃泌素释放肽(GRP)具有高亲和力的受体.BIM 189是蛙皮素的新型多肽拮抗剂,而BIM 187是一种蛙皮素激动剂.
体外实验:BIM 189是豚鼠和3T3细胞系统中已知的最有效的蛙皮素拮抗剂之一,对大鼠有40％的部分激动剂活性.激动作用的丧失可能是由于氯的吸电子效应而不是氯的大小,因为更大的Na114取代没有影响激动剂活性[2].
在体实验:4 μg/kg的BIM 187在30分钟时显著降低食物摄取,但不改变6个小时的总食物摄取.10 mg/kg以及高剂量20 mg/kg的BIM 189对食物摄入没有影响.BIM 189选择性地减少蛙皮素诱发的饱足感,但对BIM 187诱导的饱满感没有影响[2].
临床试验:截至目前,BIM 189仍处于临床前开发阶段.
参考文献：
[1] Coy D, Wang LH, Jiang NY, Jensen R. Short chain bombesin pseudopeptides with potent bombesin receptor antagonist activity in rat and guinea pig pancreatic acinar cells. Eur J Pharmacol. 1990 Nov 6;190(1-2):31-8.
[2] Laferrère B,Leroy F,Bonhomme G,Le Gall A,Basdevant A,Guy-Grand B. Effects of bombesin, of a new bombesin agonist (BIM 187) and a new antagonist (BIM 189) on food intake in rats, in relation to cholecystokinin. Eur J Pharmacol.1992 Apr 29;215(1):23-8.
| Physical Appearance | White lyophilised solid |
| Storage | Store at -20°C |
| M.Wt | 1137.73 |
| Cas No. | 142062-55-3 |
| Formula | C56H73ClN14O10 |
| Solubility | Soluble to 2 mg/ml in 20% acetonitrile |
| Chemical Name | (S)-N1-((2S,5S,8S,14S,17S,20S)-8-((1H-imidazol-4-yl)methyl)-1-amino-2-(4-chlorobenzyl)-21-(1H-indol-3-yl)-5-isobutyl-14-isopropyl-17-methyl-1,4,7,10,13,16,19-heptaoxo-3,6,9,12,15,18-hexaazahenicosan-20-yl)-2-((R)-2-amino-3-phenylpropanamido)pentanediamide |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC=C(C=C1)C[C@@H](C(N)=O)NC([C@H](CC(C)C)NC([C@H](CC2=CNC=N2)NC(CNC([C@H](C(C)C)NC([C@H](C)NC([C@H](CC3=CNC4=CC=CC=C34)NC([C@H](CCC(N)=O)NC([C@@H](CC5=CC=CC=C5)N)=O)=O)=O)=O)=O)=O)=O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
