BIM 187Bombesin/GRP receptor agonist CAS# 137734-88-4 |
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Quality Control & MSDS
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| Cas No. | 137734-88-4 | SDF | Download SDF |
| PubChem ID | 5748481 | Appearance | Powder |
| Formula | C53H76N14O10 | M.Wt | 1069.27 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | [D-Phe<sup>1</sup>,Leu<sup>8,9</sup>]litorin-NH<sub>2</sub> | ||
| Solubility | Soluble to 2 mg/ml in 20% acetonitrile | ||
| Sequence | FQWAVGHLL (Modifications: Phe-1 = D-Phe, Leu-9 = C-terminal amide) | ||
| Chemical Name | (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]pentanediamide | ||
| SMILES | CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1C=NC=N1)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CCC(=O)N)NC(=O)C(CC4=CC=CC=C4)N | ||
| Standard InChIKey | ZJPVMZDISQCAJV-MNNQHMEFSA-N | ||
| Standard InChI | InChI=1S/C53H76N14O10/c1-28(2)19-39(46(56)70)64-51(75)40(20-29(3)4)65-52(76)42(23-34-25-57-27-60-34)62-44(69)26-59-53(77)45(30(5)6)67-47(71)31(7)61-50(74)41(22-33-24-58-37-16-12-11-15-35(33)37)66-49(73)38(17-18-43(55)68)63-48(72)36(54)21-32-13-9-8-10-14-32/h8-16,24-25,27-31,34,36,38-42,45,58H,17-23,26,54H2,1-7H3,(H2,55,68)(H2,56,70)(H,59,77)(H,61,74)(H,62,69)(H,63,72)(H,64,75)(H,65,76)(H,66,73)(H,67,71)/t31-,34?,36+,38-,39-,40-,41-,42-,45-/m0/s1 | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Bombesin/GRP receptor agonist that reduces food intake following i.p. administration. |
BIM 187 Dilution Calculator
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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.
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Effects of bombesin, of a new bombesin agonist (BIM187) and a new antagonist (BIM189) on food intake in rats, in relation to cholecystokinin.[Pubmed:1516647]
Eur J Pharmacol. 1992 Apr 29;215(1):23-8.
To study the mechanism by which bombesin induces satiety, we studied the effect of two new peptides, BIM187, a bombesin agonist, and BIM189, a bombesin antagonist, on food intake in rats fed 6 h a day. BIM187 at 4 micrograms/kg, significantly reduced food intake at 30 min, but did not change the total 6-h food intake. BIM189 (10 mg/kg), had no effect on food intake when administered alone, even at high doses (20 mg/kg). BIM189 selectively reduced bombesin-induced satiety but had no effect on satiety induced by BIM187. To examine the extent to which the satiety effect of bombesin or related peptides depends on the release of cholecystokinin (CCK), we studied the ability of CCK antagonists, BIM18216 and L364718, to reduce satiety induced by bombesin and BIM187. Neither BIM18216 nor L364718 alone had an effect on the 30-min food intake. They were not able to reverse the effect of bombesin on food intake. In our model, bombesin seems to act on satiety by a mechanism independent of CCK.
