[CAS NO. 871362-31-1]  CTEP (RO4956371)

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PRODUCTS SPECIFICATIONS [871362-31-1]

Catalog
SLK-S2861
Brand
Selleck
CAS
871362-31-1

DESCRIPTION [871362-31-1]

Overview

MDLMFCD22665726
Molecular Weight391.77
Molecular FormulaC19H13ClF3N3O
SMILESCC=1N(C(C)=NC1C#CC=2C=C(Cl)N=CC2)C3=CC=C(OC(F)(F)F)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.5525 mL12.7626 mL25.5252 mL
5 mM0.5105 mL2.5525 mL5.1050 mL
10 mM0.2553 mL1.2763 mL2.5525 mL
50 mM0.0511 mL0.2553 mL0.5105 mL

Description

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

Targets

mGlu5 [1]
2.2 nM

In vitro

CTEP inhibits quisqualate-induced Ca mobilization with an IC50 of 11.4 nM and [H]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.

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 [H]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. 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.


Synonyms

Pyridine, 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-
Pyridine, 2-chloro-4-[[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-
2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]pyridine
2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine