BIM 23127 |
| Katalog-Nr.GC11620 |
Antagonist des Neuromedin-B-Rezeptors
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 160161-61-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
| Cas No. | 160161-61-5 | SDF | |
| Canonical SMILES | CC([C@@]1([H])/C(O)=N/[C@@](/C(O)=N/[C@](C(O)=N)([H])CC2=CC3=CC=CC=C3C=C2)([H])CSSC[C@@](/N=C(O)/[C@@](N)([H])CC4=CC5=CC=CC=C5C=C4)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/1)([H])CCCN)([H])CC6=CNC7=CC=CC=C67)([H])CC8=CC=C(O)C=C8)C | ||
| Formula | C62H71N11O9S2 | M.Wt | 1178.43 |
| Löslichkeit | Soluble to 2 mg/ml in 20% acetonitrile | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.8486 mL | 4.2429 mL | 8.4859 mL |
| 5 mM | 0.1697 mL | 0.8486 mL | 1.6972 mL |
| 10 mM | 0.0849 mL | 0.4243 mL | 0.8486 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *