Ici 216140
Code | Size | Price |
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TAR-T25522-5mg | 5mg | £1,042.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
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Documents
Further Information
Bioactivity:
ICI 216140 is a GRP/bombesin receptor 2 antagonist (IC50: 2 nM in vitro). At 2 mg/kg, it can decrease bombesin-stimulated pancreatic amylase secretion in rats. At 1 mM, it has been proved to attenuate bombesin-stimulated increases in blood pressure in rats.
CAS:
124001-41-8
Formula:
C45H65N13O8
Molecular Weight:
916.098
Purity:
0.98
SMILES:
CC(C)C[C@H](N(C)C(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(C)C)C(C)C)C(N)=O
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. PubMed PMID: 8813645.
2. Ryan RR, Daniel JL, Cowan A. Two bombesin analogues discriminate between neuromedin B- and bombesin-induced calcium flux in a lung cancer cell line. Peptides. 1993 Nov-Dec;14(6):1231-5. PubMed PMID: 8134305.
3. Camble R, Cotton R, Dutta AS, Garner A, Hayward CF, Moore VE, Scholes PB. N-isobutyryl-His-Trp-Ala-Val-D-Ala-His-Leu-NHMe (ICI 216140) a potent in vivo antaconist analogue of bombesin/gastrin releasing peptide (BN/GRP) derived from the C-terminal sequence lacking the final methionine residue. Life Sci. 1989;45(17):1521-7. PubMed PMID: 2555638.
4. Zogovic B, Pilowsky PM. Intrathecal bombesin is sympathoexcitatory and pressor in rat. Am J Physiol Regul Integr Comp Physiol. 2011 Nov;301(5):R1486-94. doi: 10.1152/ajpregu.00297.2011. Epub 2011 Aug 17. PubMed PMID: 21849634.