BIM 189

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 . 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. Clinical trial: Up to now, BIM 189 is still in the preclinical development stage.

Product information

CAS Number: 142062-55-3

Molecular Weight: 1137.72

Formula: C56H73ClN14O10

Chemical Name: (2S)-2-[(2R)-2-amino-3-phenylpropanamido]-N-[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-1-{[(1S)-1-carbamoyl-2-(4-chlorophenyl)ethyl]carbamoyl}-3-methylbutyl]carbamoyl}-2-(1H-imidazol-4-yl)ethyl]carbamoyl}methyl)carbamoyl]-2-methylpropyl]carbamoyl}ethyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]pentanediamide

Smiles: C[C@H](NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](N)CC1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1C=CC(Cl)=CC=1)C(N)=O

InChiKey: XJWMPWLZAVKSPK-UYBYNCNQSA-N

InChi: InChI=1S/C56H73ClN14O10/c1-30(2)21-43(54(79)68-42(49(60)74)23-34-15-17-36(57)18-16-34)69-55(80)45(25-37-27-61-29-64-37)66-47(73)28-63-56(81)48(31(3)4)71-50(75)32(5)65-53(78)44(24-35-26-62-40-14-10-9-13-38(35)40)70-52(77)41(19-20-46(59)72)67-51(76)39(58)22-33-11-7-6-8-12-33/h6-18,26-27,29-32,39,41-45,48,62H,19-25,28,58H2,1-5H3,(H2,59,72)(H2,60,74)(H,61,64)(H,63,81)(H,65,78)(H,66,73)(H,67,76)(H,68,79)(H,69,80)(H,70,77)(H,71,75)/t32-,39+,41-,42-,43-,44-,45-,48-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.