CTEP (RO4956371)

Catalog No.S2861

CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.

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CTEP (RO4956371) Chemical Structure

CTEP (RO4956371) Chemical Structure
Molecular Weight: 391.77

Validation & Quality Control

Quality Control & MSDS

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CTEP (RO4956371) is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.
Targets mGluR5
IC50 2.2 nM [1]
In vitro CTEP inhibits quisqualate-induced Ca2+ mobilization with an IC50 of 11.4 nM and [3H]IP accumulation with an IC50 of 6.4 nM in HEK293 cells stably expressing human mGlu5. CTEP inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1 nM in HEK293 cells stably expressing human mGlu5. [1]
In vivo CTEP is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in the Vogel conflict drinking test in rat, whereas it has no effect at lower doses. The half-life of CTEP (oral) is 18 h, and the B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice. After single oral doses of 4.5 and 8.7 mg/kg CTEP formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice is rapidly absorbed and achieves close to maximal exposure after approximately 30 min. Chronic administration in adult mice with a dose of 2 mg/kg p.o. every 48 h for 2 months reaches a minimal CTEP brain exposure of 240 ng/g. CTEP fully displaces [3H]ABP688 in mouse brain regions known to express mGlu5, and 50% displacement is achieved with doses producing an average compound concentration of 77.5 ng/g measured in whole brain homogenate. [1] CTEP (2 mg/kg p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (2 mg/kg p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse. [2]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Study: [1]

Animal Models Male Sprague-Dawley rats
Formulation 0.9% NaCl (w/v) and 0.3% Tween 80 (v/v) solution
Dosages 1.0 mg/kg
Administration orally
Solubility 30% propylene glycol, 5% Tween 80, 65% D5W, , 6 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

[1] Lindemann L, et al. J Pharmacol Exp Ther, 2011, 339(2), 474-486.

[2] Michalon A, et al. Neuron, 2012, 74(1), 49-56.

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01322802 Recruiting Stage III Ovarian Epithelial Cancer|Stage III Ovarian Germ Cell Tumor|Stage IV Ovarian Epithelial Cancer|Stage IV Ovarian Germ Cell Tumor FredHutchinsonCancerResearchCenter|Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium|NationalCancerInstitute(NCI) 2012-03 Phase 1
NCT01536067 Recruiting Waldenstr枚m Macroglobulinemia RoswellParkCancerInstitute|NationalCancerInstitute(NCI) 2012-04 Phase 2
NCT01606241 Recruiting Recurrent Breast Cancer|Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Ovarian Germ Cell Tumor|Recurrent Primary Peritoneal Cavity Cancer etc. MayoClinic 2012-07 Phase 1
NCT01632332 Recruiting HER2-positive Breast Cancer|Male Breast Cancer|Stage II Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer MayoClinic|TapImmune,Inc. 2012-07 Phase 1
NCT01729884 Recruiting HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer FredHutchinsonCancerResearchCenter|Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium|NationalCancerInstitute(NCI) 2012-12 Phase 2

Chemical Information

Download CTEP (RO4956371) SDF
Molecular Weight (MW) 391.77
Formula

C19H13ClF3N3O

CAS No. 871362-31-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 78 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 10 mg/mL (25 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W, 6 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Pyridine, 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-

Research Area

Tech Support & FAQs

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