BIM 23127Antagonist of neuromedin B receptor CAS# 160161-61-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 160161-61-5 | SDF | Download SDF |
| PubChem ID | 90488717 | Appearance | Powder |
| Formula | C62H71N11O9S2 | M.Wt | 1178.43 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 2 mg/ml in 20% acetonitrile | ||
| Chemical Name | (4R,7S,10S,13R,16S,19R)-N-[(2R)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-19-[[(2R)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-10-(3-aminopropyl)-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | ||
| SMILES | CC(C)C1C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)N)C(=O)NC(CC7=CC8=CC=CC=C8C=C7)C(=O)N | ||
| Standard InChIKey | GLVLDCUADDSQSK-JGRJXKJCSA-N | ||
| Standard InChI | InChI=1S/C62H71N11O9S2/c1-35(2)54-62(82)72-53(60(80)68-49(55(65)75)30-38-18-22-40-11-4-6-13-42(40)27-38)34-84-83-33-52(71-56(76)46(64)28-37-17-21-39-10-3-5-12-41(39)26-37)61(81)69-50(29-36-19-23-44(74)24-20-36)58(78)70-51(31-43-32-66-47-15-8-7-14-45(43)47)59(79)67-48(16-9-25-63)57(77)73-54/h3-8,10-15,17-24,26-27,32,35,46,48-54,66,74H,9,16,25,28-31,33-34,63-64H2,1-2H3,(H2,65,75)(H,67,79)(H,68,80)(H,69,81)(H,70,78)(H,71,76)(H,72,82)(H,73,77)/t46-,48+,49-,50+,51-,52+,53+,54+/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Neuromedin B receptor (NMB-R, BB1) antagonist (Ki values are 20.9 and > 10000 nM for NMB and gastrin-releasing peptide receptors respectively). Selectively blocks NMB-suppressed glucose intake in vivo. Also a potent urotensin-II receptor antagonist (pA2 = 7.5 - 7.7) and displays affinity for somatostatin and μ-opioid receptors. |
BIM 23127 Dilution Calculator
BIM 23127 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 0.8486 mL | 4.2429 mL | 8.4859 mL | 16.9717 mL | 21.2147 mL |
| 5 mM | 0.1697 mL | 0.8486 mL | 1.6972 mL | 3.3943 mL | 4.2429 mL |
| 10 mM | 0.0849 mL | 0.4243 mL | 0.8486 mL | 1.6972 mL | 2.1215 mL |
| 50 mM | 0.017 mL | 0.0849 mL | 0.1697 mL | 0.3394 mL | 0.4243 mL |
| 100 mM | 0.0085 mL | 0.0424 mL | 0.0849 mL | 0.1697 mL | 0.2121 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Ki: 20.9 nM for neuromedin B receptors
Bombesin (BN) belongs to a family of neuropeptides whose members, as well as their respective receptors, are widely distributed throughout the mammalian central nervous system (CNS). BN and its related peptides modulate behaviors such as spontaneous activities and feeding. BIM 23127 (D-Nal-cyclo[Cys-Tyr-D-Trp-Orn-Val-Cys]-Nal-NH2) is a neuromedin B receptor antagonist.
In vitro: BIM 23127 was reported to potenly give antagonist effect on neuromedin B receptor (Ki = 20.9 nM). In addition, BIM 23127 was also found to be a selective neuromedin B receptor antagonist (> 10000 nM for gastrin-releasing peptide receptors) [2].
In vivo: Prior administration of 100 nmol/kg of BIM 23127 completely blocked the glucose intake suppression produced by neuromedin B. BIM 23127 also completely blocked suppression of intake produced by neuromedin B rather than by neuromedin C. These results suggest an independent role for neuromedin B receptors in suppression of food intake by bombesin-like peptides [3].
Clinical trial: Up to now, BIM 23127 is still in the preclinical development stage.
Reference:
[1] Ladenheim EE, Taylor JE, Coy DH, Moran TH. Blockade of feeding inhibition by neuromedin B using a selective receptor antagonist. Eur J Pharmacol. 1994 Dec 12;271(1):R7-9.
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The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors.[Pubmed:12770925]
Br J Pharmacol. 2003 May;139(2):203-7.
The functional activity of the peptidic neuromedin B receptor antagonist BIM-23127 was investigated at recombinant and native urotensin-II receptors (UT receptors). Human urotensin-II (hU-II) promoted intracellular calcium mobilization in HEK293 cells expressing the human UT (hUT) or rat UT (rUT) receptors with pEC(50) values of 9.80+/-0.34 (n=6) and 9.06+/-0.32 (n=4), respectively. While BIM-23127 alone had no effect on calcium responses in either cell line, it was a potent and competitive antagonist at both hUT (pA(2)=7.54+/-0.14; n=3) and rUT (pA(2)=7.70+/-0.05; n=3) receptors. Furthermore, BIM-23127 reversed hU-II-induced contractile tone in the rat-isolated aorta with a pIC(50) of 6.66+/-0.04 (n=4). In conclusion, BIM- 23127 is the first hUT receptor antagonist identified to date and should not be considered as a selective neuromedin B receptor antagonist.
