ICI 216140 is a GRP/bombesin receptor 2 antagonist (IC50 = 2 nM in vitro). At 2 mg/kg, it can reduce bombesin-stimulated pancreatic amylase secretion in rats. At 1 mM, it has been shown to attenuate bombesin-stimulated increases in blood pressure in rats. Bombesin is a peptide, originally isolated from the skin of the European fire-bellied toad, with pressor and sympathoexcitatory activity. Its three receptors are distributed throughout the central and peripheral nervous system and are involved in gastric acid secretion, emotional response, temperature control, learning, and memory. Neuromedin B and gastrin-releasing peptide (GRP) are mammalian homologs of bombesin.
MedKoo Cat#: 597417
Name: Ici 216140
CAS#: 124001-41-8
Chemical Formula: C45H65N13O8
Exact Mass: 915.5079
Molecular Weight: 916.10
Elemental Analysis: C, 59.00; H, 7.15; N, 19.88; O, 13.97
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 2.0 | 2.18 | |
| DMSO | 2.0 | 2.18 | |
| PBS (pH 7.2) | 10.0 | 10.92 |
The following data is based on the product molecular weight 916.10 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
