Home Neuronal Signaling GluR antagonist CTEP (RO4956371)

research use only

CTEP (RO4956371) GluR antagonist

Cat.No.S2861

CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and it shows >1000-fold selectivity over other mGlu receptors.
CTEP (RO4956371) GluR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 391.77

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 391.77 Formula

C19H13ClF3N3O

 Storage (From the date of receipt)
CAS No. 871362-31-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(N=C(N1C2=CC=C(C=C2)OC(F)(F)F)C)C#CC3=CC(=NC=C3)Cl

Solubility

In vitro
Batch:

DMSO : 78 mg/mL ( (199.09 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Mechanism of Action

Targets/IC50/Ki
mGlu5 [1]
2.2 nM
In vitro
In HEK293 cells stably expressing human mGlu5, CTEP (RO4956371) inhibits quisqualate-induced Ca2+ mobilization with an IC50 of 11.4 nM and [3H]IP accumulation with an IC50 of 6.4 nM. It also inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1 nM. [1]
In vivo
CTEP (RO4956371) is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. It 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 this compound (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 formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice, it 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 brain exposure of 240 ng/g. It 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] At 2 mg/kg p.o. bid, it achieves uninterrupted mGlu5 occupancy per 48 hours in mice. Treatment with this compound (2 mg/kg p.o.) corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse. [2]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05915208 Recruiting
Histiocytosis|Langerhans Cell Histiocytosis|Erdheim-Chester Disease|Rosai Dorfman Disease|Xanthogranuloma|Malignant Histiocytoses
University of Alabama at Birmingham
 September 1 2022 --
NCT02424916 Completed
Metastatic Melanoma
Nantes University Hospital|UMR892
 May 26 2015 Phase 1|Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Frequently Asked Questions

Question 1:
Do you have advice for its administration in mouse via injection?

Answer:
The IP formula for S2861 is 2% DMSO+40% PEG300+2% Tween-80 +H2O.

Signaling Pathway Map