BIM 187
目录号 : GC15165Bombesin/GRP receptor agonist
Cas No.:137734-88-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bombesin has common effects on the gastrointestinal tract and feeding behavior. Bombesin acts on two types of receptors including one with high affinity for neuromedin B and another with high affinity for bombesin and gastrin-releasing peptide (GRP). BIM 187is a new peptide of bombesin while BIM 189 is a potent bombesin antagonis.
In vitro: Bombesin stimulates mainly the bombesin high-affinity receptor, and BIM 187 ([D-Phe I ,Leu 8'9 ]litorin-NHe), a new bombesin agonist, stimulates the bombesin/GRP receptor type. [2].
In vivo: To study the mechanism by which bombesin induces satiety, we studied the effect of BIM187 on food intake in rats fed 6 h a day. BIM 187 at 4 μg/kg, reduced food intake at 30 min significantly, but did not change the total 6-h food intake. BIM 189 (10 mg/kg), had no effect on food intake, even at high doses (20 mg/kg). BIM 189 selectively reduced bombesin-induced satiety but had no effect on satiety induced by BIM 187 [2].
Clinical trial: Up to now, BIM 187 is still in the preclinical development stage.
Reference:
[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 (BIM187) and a new antagonist (BIM189) on food intake in rats, in relation to cholecystokinin. Eur J Pharmacol. 1992 Apr 29;215(1):23-8.
Cas No. | 137734-88-4 | SDF | |
化学名 | (S)-N1-((2S,5S,8S,14S,17S,20S)-14-(((R)-4H-imidazol-4-yl)methyl)-20-carbamoyl-1-(1H-indol-3-yl)-17-isobutyl-8-isopropyl-5,22-dimethyl-3,6,9,12,15,18-hexaoxo-4,7,10,13,16,19-hexaazatricosan-2-yl)-2-((R)-2-amino-3-phenylpropanamido)pentanediamide | ||
Canonical SMILES | O=C([C@H](CC(C)C)NC([C@H](C[C@H]1N=CN=C1)NC(CNC([C@H](C(C)C)NC([C@H](C)NC([C@H](CC2=CNC3=CC=CC=C23)NC([C@H](CCC(N)=O)NC([C@@H](CC4=CC=CC=C4)N)=O)=O)=O)=O)=O)=O)=O)N[C@H](C(N)=O)CC(C)C | ||
分子式 | C53H76N14O10 | 分子量 | 1069.27 |
溶解度 | Soluble to 2 mg/ml in Water | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 0.9352 mL | 4.6761 mL | 9.3522 mL |
5 mM | 0.187 mL | 0.9352 mL | 1.8704 mL |
10 mM | 0.0935 mL | 0.4676 mL | 0.9352 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
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