Name: CTEP (RO4956371)
Brand: Selleck Chemicals
SKU: S2861
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: S286101 DMSO]78 mg/mL]false]Ethanol]78 mg/mL]false]Water]Insoluble]false Purity: 99.3%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS/MSDS
Datasheet

99.3

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other GluR Inhibitors	pomaglumetad (LY404039) O-Phospho-L-serine (S)-Glutamic acid CNQX VU 0357121 MPEP ADX-47273 Xanthurenic Acid L-Glutamic acid monosodium salt Capric acid

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

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Average weight of animals: g

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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

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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.

Chemical Information, Storage & Stability

Molecular Weight	391.77	Formula	C₁₉H₁₃ClF₃N₃O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	871362-31-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	CC1=C(N=C(N1C2=CC=C(C=C2)OC(F)(F)F)C)C#CC3=CC(=NC=C3)Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	mGlu5 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.
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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21849627/ [2] https://pubmed.ncbi.nlm.nih.gov/22500629/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-28)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02839707	ACTIVE_NOT_RECRUITING	Fallopian Tube High Grade Serous Adenocarcinoma; Ovarian High Grade Serous Adenocarcinoma; Ovarian Seromucinous Carcinoma; Primary Peritoneal High Grade Serous Adenocarcinoma; Recurrent Fallopian Tube Carcinoma; Recurrent Fallopian Tube Clear Cell Adenocarcinoma; Recurrent Fallopian Tube Endometrioid Adenocarcinoma; Recurrent Fallopian Tube Undifferentiated Carcinoma; Recurrent Ovarian Carcinoma; Recurrent Ovarian Clear Cell Adenocarcinoma; Recurrent Ovarian Endometrioid Adenocarcinoma; Recurrent Ovarian Undifferentiated Carcinoma; Recurrent Platinum-Resistant Fallopian Tube Carcinoma; Recurrent Platinum-Resistant Ovarian Carcinoma; Recurrent Platinum-Resistant Primary Peritoneal Carcinoma; Recurrent Primary Peritoneal Carcinoma; Recurrent Primary Peritoneal Clear Cell Adenocarcinoma; Recurrent Primary Peritoneal Endometrioid Adenocarcinoma; Recurrent Primary Peritoneal Undifferentiated Carcinoma	National Cancer Institute (NCI)	2017-06-23	PHASE2; PHASE3
NCT05915208	Recruiting	Histiocytosis\|Langerhans Cell Histiocytosis\|Erdheim-Chester Disease\|Rosai Dorfman Disease\|Xanthogranuloma\|Malignant Histiocytoses	University of Alabama at Birmingham	2022-09-01	--
NCT01281852	COMPLETED	Cervical Adenocarcinoma; Cervical Adenosquamous Carcinoma; Cervical Squamous Cell Carcinoma, Not Otherwise Specified; Recurrent Cervical Carcinoma; Stage IVB Cervical Cancer AJCC v6 and v7	National Cancer Institute (NCI)	2011-03-14	PHASE1
NCT00989651	COMPLETED	Fallopian Tube Carcinoma; Fallopian Tube Carcinosarcoma; Fallopian Tube Clear Cell Adenocarcinoma; Fallopian Tube Endometrioid Adenocarcinoma; Fallopian Tube Mucinous Adenocarcinoma; Fallopian Tube Serous Neoplasm; Fallopian Tube Transitional Cell Carcinoma; Fallopian Tube Undifferentiated Carcinoma; Ovarian Brenner Tumor; Ovarian Carcinoma; Ovarian Carcinosarcoma; Ovarian Clear Cell Adenocarcinoma; Ovarian Endometrioid Adenocarcinoma; Ovarian Mucinous Adenocarcinoma; Ovarian Seromucinous Tumor; Ovarian Serous Adenocarcinoma; Ovarian Transitional Cell Carcinoma; Ovarian Undifferentiated Carcinoma; Primary Peritoneal Carcinoma; Primary Peritoneal Serous Adenocarcinoma; Stage IIA Fallopian Tube Cancer AJCC v6 and v7; Stage IIA Ovarian Cancer AJCC V6 and v7; Stage IIB Fallopian Tube Cancer AJCC v6 and v7; Stage IIB Ovarian Cancer AJCC v6 and v7; Stage IIC Fallopian Tube Cancer AJCC v6 and v7; Stage IIC Ovarian Cancer AJCC v6 and v7; Stage IIIA Fallopian Tube Cancer AJCC v7; Stage IIIA Ovarian Cancer AJCC v6 and v7; Stage IIIA Primary Peritoneal Cancer AJCC v7; Stage IIIB Fallopian Tube Cancer AJCC v7; Stage IIIB Ovarian Cancer AJCC v6 and v7; Stage IIIB Primary Peritoneal Cancer AJCC v7; Stage IIIC Fallopian Tube Cancer AJCC v7; Stage IIIC Ovarian Cancer AJCC v6 and v7; Stage IIIC Primary Peritoneal Cancer AJCC v7; Stage IV Fallopian Tube Cancer AJCC v6 and v7; Stage IV Ovarian Cancer AJCC v6 and v7; Stage IV Primary Peritoneal Cancer AJCC v7	National Cancer Institute (NCI)	2009-10-28	PHASE1
NCT02424916	Completed	Metastatic Melanoma	Nantes University Hospital\|UMR892	2015-05-26	Phase 1\|Phase 2
NCT01074411	COMPLETED	Fallopian Tube Clear Cell Adenocarcinoma; Fallopian Tube Endometrioid Adenocarcinoma; Fallopian Tube Mucinous Adenocarcinoma; Fallopian Tube Serous Adenocarcinoma; Fallopian Tube Transitional Cell Carcinoma; Ovarian Brenner Tumor; Ovarian Clear Cell Adenocarcinoma; Ovarian Clear Cell Cystadenocarcinoma; Ovarian Endometrioid Adenocarcinoma; Ovarian Mucinous Adenocarcinoma; Ovarian Mucinous Cystadenocarcinoma; Ovarian Seromucinous Carcinoma; Ovarian Serous Adenocarcinoma; Ovarian Serous Cystadenocarcinoma; Ovarian Transitional Cell Carcinoma; Recurrent Fallopian Tube Carcinoma; Recurrent Ovarian Carcinoma; Recurrent Primary Peritoneal Carcinoma; Undifferentiated Fallopian Tube Carcinoma; Undifferentiated Ovarian Carcinoma	National Cancer Institute (NCI)	2010-04-05	PHASE1

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Handling Instructions

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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.

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CTEP (RO4956371) GluR antagonist

Chemical Structure

Molecular Weight: 391.77