BIM 189 |
| Catalog No.GC14279 |
Bombesin antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 142062-55-3
Sample solution is provided at 25 µL, 10mM.
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IC50: 10.4 nM for rat pancreas; 2.4 nM for Guinea pig pancreas
Bombesin has common effects on the gastrointestinal tract and feeding behavior. Bombesin acts on two types of receptors: one with high affinity for neuromedin B and another with high affinity for bombesin and gastrin-releasing peptide (GRP). BIM 189 is a a new peptide of bombesin antagonis, while BIM 187 is a bombesin agonist.
In vitro: BIM 189 was one of the most potent bombesin antagonists known in the guinea pig and 3T3 cell systems but has 40% partial agonist activity in the rat. Loss of agonism might be attributed to the Cl electron withdrawing effects rather than the size of the Cl since far larger Na114 substitutions did not effect agonist activity [2].
In vivo: BIM 187 at 4 μg/kg, significantly reduced food intake at 30 min in rat, but did not change the total 6-h food intake. BIM 189 (10 mg/kg), had no effect on food intake when administered alone, 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 189 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 (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.
| Cas No. | 142062-55-3 | SDF | |
| 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 | ||
| 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 | ||
| Formula | C56H73ClN14O10 | M.Wt | 1137.73 |
| Solubility | Soluble to 2 mg/ml in 20% acetonitrile | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.8789 mL | 4.3947 mL | 8.7894 mL |
| 5 mM | 0.1758 mL | 0.8789 mL | 1.7579 mL |
| 10 mM | 0.0879 mL | 0.4395 mL | 0.8789 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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