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BIM 23042 TFA

Names

[ CAS No. ]:
111857-96-6

[ Name ]:
BIM 23042 TFA

[Synonym ]:
1,2-Dithia-5,8,11,14,17-pentaazacycloeicosane-4-carboxamide, 10-(4-aminobutyl)-N-[(1R)-2-amino-1-(2-naphthalenylmethyl)-2-oxoethyl]-19-[[(2R)-2-amino-3-(2-naphthalenyl)-1-oxopropyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-7-(1-methylethyl)-6,9,12,15,18-pentaoxo-, (4R,7S,10S,13R,16S,19R)-
(4R,7S,10S,13R,16S,19R)-10-(4-Aminobutyl)-N-[(2R)-1-amino-3-(2-naphthyl)-1-oxo-2-propanyl]-19-{[(2R)-2-amino-3-(2-naphthyl)propanoyl]amino}-16-(4-hydroxybenzyl)-13-(1H-indol-3-ylmethyl)-7-isopropyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide

Biological Activity

[Description]:

BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release[1][2][3].

[Related Catalog]:

Research Areas >> Metabolic Disease
Signaling Pathways >> GPCR/G Protein >> Bombesin Receptor
Research Areas >> Neurological Disease

[In Vitro]

BIM 23042 (5 μM) 在 huNMBR 细胞中竞争性抑制 Neuromedin B 诱导的 [3H] 花生四烯酸释放，Ki 为 49 nM[1]。

[In Vivo]

BIM 23042 (10μg; 静脉给药; 单次推注) 可减轻神经源性肿胀和热和机械致敏[2]。 Animal Model: Mice were 25-30 g male C57BL/6[2] Dosage: 10 μg Administration: IV; a single bolus Result: Attenuated neurogenic swelling and thermal and mechanical sensitization.

[References]

[1]. R R Ryan, et al. 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.  

[2]. Santosh K Mishra, et al. A nociceptive signaling role for neuromedin B. J Neurosci. 2012 Jun 20;32(25):8686-95.  

[3]. M Orbuch, et al. Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues. Mol Pharmacol. 1993 Oct;44(4):841-50.  

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
1554.2±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C62H73N11O9S2

[ Molecular Weight ]:
1192.452

[ Flash Point ]:
893.7±34.3 °C

[ Exact Mass ]:
1191.503418

[ PSA ]:
412.45000

[ LogP ]:
6.00

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.709

Related Compounds