| BIM 187Bombesin/GRP receptor agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 137734-88-4 | SDF | Download SDF |
| Chemical Name | (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 | ||
| Formula | C53H76N14O10 | M.Wt | 1069.27 |
| Solubility | Soluble to 2 mg/ml in H2O | Storage | Store at -20°C |
| Physical Appearance | White lyophilised solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
