BIBP 3226 trifluoroacetate |
| Katalog-Nr.GC11074 |
BIBP 3226 Trifluoracetat ist ein potenter und selektiver Neuropeptid Y Y1 (NPY Y1) und Neuropeptid FF (NPFF) Rezeptorantagonist mit Kis von 1,1, 79 und 108 nM fÜr rNPY Y1, hNPFF2 bzw. rNPFF.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1068148-47-9
Sample solution is provided at 25 µL, 10mM.
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BIBP 3226 trifluoroacetate is a non-peptide neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist with Ki values of 1.1, 79, 108 for rNPY Y1, hNPFF2, rNPFF, respectively.
Neuropeptide Y Y1 receptors (NPY Y1) involve in the regulation of exploratory behaviour and anxiety. Neuropeptide FF (NPFF) is a part of a neurotransmitter system functioning as a modulator of endogenous opioid functions [1].
BIBP 3226 was able to compete for the specific NPFF binding expressed in CHO cells as well as in rat dorsal spinal cord. In hNPFF2 receptors transfected cells, BIBP 3226 (10mM) is able to antagonize the inhibition of forskolin-stimulated cyclic AMP production induced by NPFF (10nM) in a concentration-dependent manner [2].
In male Wistar rats, BIBP3226 at the dose of 5 mg caused an anxiogenic-like effect while the lower dose was ineffective. While, the overall locomotory activity didn’t change in all treatment groups [1]. In mice model, BIBP3226 (5nmol) injected into the third ventricle completely antagonized the hypothermic effects of NPFF (30nmol) and NPVF (30nmol). In the mouse tail-flick assay, BIBP3226 (5nmol) prevented the anti-morphine actions of NPFF (10nmol). Also, in urethane-anaesthetized rats, BIBP3226 (500nmol/kg) significantly reduced the mean arterial blood pressure induced by NPFF (200nmol/kg) and NPVF (200nmol/kg) [3].
References:
[1]. Kask A1, R?go L, Harro J. Anxiogenic-like effect of the neuropeptide Y Y1 receptor antagonist BIBP3226: antagonism with diazepam. Eur J Pharmacol, 1996, 317(2-3): R3-4.
[2]. Mollereau C1, Gouardères C, Dumont Y, et al. Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226. Br J Pharmacol, 2001, 133(1): 1-4.
[3]. Fang Q1, Guo J, He F, et al. In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist. Peptides, 2006, 27(9): 2207-2213.
| Cas No. | 1068148-47-9 | SDF | |
| Chemical Name | (R)-2-(2,2-diphenylacetamido)-5-guanidino-N-(4-hydroxybenzyl)pentanamide bis(2,2,2-trifluoroacetate) | ||
| Canonical SMILES | FC(F)(C(O)=O)F.OC1=CC=C(C=C1)CNC([C@@H](CCCNC(N)=N)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O.FC(F)(C(O)=O)F | ||
| Formula | C27H31N5O3.2CF3CO2H | M.Wt | 701.61 |
| Löslichkeit | <7.02mg/ml in Water; <70.16mg/ml in DMSO | Storage | Store at -20°C, protect from light |
| 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. |
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| 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 | 1.4253 mL | 7.1265 mL | 14.2529 mL |
| 5 mM | 0.2851 mL | 1.4253 mL | 2.8506 mL |
| 10 mM | 0.1425 mL | 0.7126 mL | 1.4253 mL |
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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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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