BIM 23042
Ki: 49 ±14 nM for neuromedin B-induced endpoint in huNMBR cells
Neuromedin B, a mammalian peptide of the bombesinlike peptide family sharing amino acid homology with its amphibian counterpart ranatensin, elicits a diverse array of biological responses in central and peripheral tissues. BIM 23042 [D-Nal-Cys-Tyr- D-Trp-Lys-Val-Cys-Nal-NH2] is a selective neuromedin B antagonist.
In vitro: BIM 23042 has a l00-fold greater affinity for BB1 receptors than BB2 receptors. The submaximal mobilisation observed with neuromedin B (1 nM) was abolished by BIM 23042 but restored with a subsequently higher concentration of neuromedin B (1 μM). BIM 23042 competitively inhibited neuromedin B-induced endpoint in huNMBR cells with a Ki of 49 ±14 nM [1].
Clinical trial: Up to now, BIM 23042 is still in the preclinical development stage.
References:
[1] Ryan RR, Taylor JE, Daniel JL, Cowan A. Pharmacological profiles of two bombesin analogues in cells transfected with human neuromedin B receptors. Eur J Pharmacol. 1996 Jun 13;306(1-3):307-14.
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 1192.47 |
| Cas No. | 111857-96-6 |
| Formula | C63H73N11O9S2 |
| Solubility | ≥43.8 mg/mL in DMSO; ≥42.7 mg/mL in EtOH; ≥8.04 mg/mL in H2O with ultrasonic |
| Chemical Name | (4R,7S,10S,13R,16S,19R)-13-((1H-indol-3-yl)methyl)-N-((S)-1-amino-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-19-((R)-2-amino-3-(naphthalen-2-yl)propanamido)-10-(4-aminobutyl)-16-(4-hydroxybenzyl)-7-isopropyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaa |
| SDF | Download SDF |
| Canonical SMILES | O=C(N[C@H](CC1=CNC2=CC=CC=C21)C(N[C@@H](CCCCN)C(N[C@H]3C(C)C)=O)=O)[C@@H](NC([C@H](CSSC[C@@H](C(N[C@@H](CC4=CC(C=CC=C5)=C5C=C4)C(N)=O)=O)NC3=O)NC([C@@H](CC6=CC7=C(C=CC=C7)C=C6)N)=O)=O)CC8=CC=C(O)C=C8 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
