CTEP (RO4956371) (Synonyms: RO 4956371; mGluR5 inhibitor) |
| Katalog-Nr.GC16619 |
CTEP (RO4956371) (RO 4956371) ist ein neuartiger, lang wirkender, oral bioverfÜgbarer allosterischer Antagonist des mGlu5-Rezeptors mit einem IC50 von 2,2 nM und zeigt eine > 1000-fache SelektivitÄt gegenÜber anderen mGlu-Rezeptoren.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 871362-31-1
Sample solution is provided at 25 µL, 10mM.
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CTEP is a potent, long-acting, and orally bioavailable inhibitor of metabotropic glutamate receptor 5 (mGlu5) with IC50 value of 11.4nM [1].
CTEP is a negative allosteric modulator of mGlu5 and has inverse agonist activity. In the in vitro binding assay, CTEP binds to human, mouse and rat mGlu5 with Kd values of 1.7nM, 1.8nM and 1.5 nM, respectively. In HEK293 cells expressing mGlu5, CTEP inhibits quisqualate-induced Ca2+ mobilization and inositol phosphate accumulation with IC50 value of 11.4nM and 6.4nM, respectively. In addition, it shows an IC50 value of 40.1nM in the IP accumulation assay, demonstrating its inverse agonist activity. CTEP is proved to be a highly selective inhibitor of mGlu5. It shows no significant activity against mGlu1, mGlu2, mGlu3, mGlu4, mGlu6, mGlu7 or mGlu8 at concentration up to 10μM [1].
In the in vivo Vogel conflict drinking test, CTEP markedly increases drinking time at doses of 0.3mg/kg. In adult C57BL/6 mice brain, CTEP displaces the mGlu5 antagonist ABP688 in the regions expressing mGlu5 by 50% at dose of 77.5 ng/g [1].
References:
[1] Lindemann L, Jaeschke G, Michalon A, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. Journal of Pharmacology and Experimental Therapeutics, 2011, 339(2): 474-486.
| Kinase experiment [1]: | |
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Radioligand Binding Assays |
For all filtration radioligand binding assays, membrane preparations expressing the target receptors or receptor combinations are resuspended in radioligand binding buffer (15 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, 1.25 mM CaCl2, and 1.25 mM MgCl2, pH 7.4), and the membrane suspension is mixed with the appropriate concentrations of radioligand and nonlabeled drugs in 96-well plates in a total volume of 200 μL and incubated for 60 min at the appropriate temperature. At the end of the incubation, membranes are filtered onto Whatman Unifilter preincubated with 0.1% polyethyleneimine in wash buffer (50 mM Tris-HCl, pH 7.4) with a Filtermate 196 harvester and washed three times with ice-cold wash buffer. Radioactivity captured on the filter is quantified on a Topcount microplate scintillation counter with quenching correction after the addition of 45 μL of MicroScint 40 per well and shaking for 20 min. The concentration of membranes and incubation time is determined for each assay in pilot experiments. |
| Animal experiment: | |
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Animal models |
Adult male C57BL/6 mice model; Adult male Sprague-Dawley rats model; Fmr1 knockout mouse model |
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Dosage form |
0.01 to 3.0 mg/kg; oral gavage; for 18 hours; or 2 mg/kg per 48 hr p.o. for 2 weeks |
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Applications |
CTEP (0.1 and 0.3 mg/kg) was dose-dependently active in the stress-induced hyperthermia procedure in mice and the Vogel conflict drinking test in rats [1]. Moreover, CTEP corrected excessive protein synthesis, mGlu-long-term depression, and audiogenic seizures in the Hippocampus of Fmr1 knockout mice [2]. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Lindemann, L., Jaeschke, G., Michalon, A., Vieira, E., Honer, M., Spooren, W., Porter, R., Hartung, T., Kolczewski, S., Buttelmann, B., Flament, C., Diener, C., Fischer, C., Gatti, S., Prinssen, E. P., Parrott, N., Hoffmann, G. and Wettstein, J. G. (2011) CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 339, 474-486 2. Michalon, A., Sidorov, M., Ballard, T. M., Ozmen, L., Spooren, W., Wettstein, J. G., Jaeschke, G., Bear, M. F. and Lindemann, L. (2012) Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 74, 49-56 | |
| Cas No. | 871362-31-1 | SDF | |
| Überlieferungen | RO 4956371; mGluR5 inhibitor | ||
| Chemical Name | 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine | ||
| Canonical SMILES | CC1=C(N=C(N1C2=CC=C(C=C2)OC(F)(F)F)C)C#CC3=CC(=NC=C3)Cl | ||
| Formula | C19H13ClF3N3O | M.Wt | 391.77 |
| Löslichkeit | ≥ 19.6mg/mL in DMSO | Storage | Store 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. |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5525 mL | 12.7626 mL | 25.5252 mL |
| 5 mM | 0.5105 mL | 2.5525 mL | 5.105 mL |
| 10 mM | 0.2553 mL | 1.2763 mL | 2.5525 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 15 reference(s) in Google Scholar.)
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