CTEP

SKU: orb1300752

Description

CTEP

Research Area

Neuroscience

Key Properties

• CAS Number: 871362-31-1
• MW: 391.77
• Purity: 99.17%
• Formula: C₁₉H₁₃ClF₃N₃O
• SMILES: Cc1nc(C#Cc2ccnc(Cl)c2)c(C)n1-c1ccc(OC(F)(F)F)cc1
• Target: GluR
• Solubility: Ethanol:10 mg/mL (25.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.11 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:65 mg/mL (165.91 mM)

Bioactivity

• Target IC50:
  mGlu5:2.2 nM
• In Vivo:
  CTEP exhibits significant efficacy at doses of 0.1 mg/kg and 0.3 mg/kg for treating anxiety in mice and enhances drinking behavior in the Vogel conflict drinking test at doses of 0.3 mg/kg and 1.0 mg/kg in rats, showing no effect at lower doses. The compound demonstrates an oral half-life of 18 hours, with a brain/plasma (B/P) ratio of 2.6 in mice, indicating its penetration and persistence in brain tissue. When administered orally to adult C57BL/6 mice as a microsuspension in saline/Tween, CTEP is rapidly absorbed, reaching near-maximal levels about 30 minutes post-dosing. Chronic dosing of 2 mg/kg orally every 48 hours for two months in adult mice ensures a minimal brain concentration of 240 ng/g. CTEP effectively displaces [3H]ABP688 from mGlu5 receptors in the mouse brain, with a 50% displacement achieved at an average brain concentration of 77.5 ng/g. At a regimen of 2 mg/kg orally twice daily, CTEP maintains continuous mGlu5 receptor engagement over 48 hours. Additionally, CTEP treatment at 2 mg/kg orally corrects hippocampal dysfunction, excessive protein synthesis, and audiogenic seizures in Fmr1 knockout mice, showcasing its potential in addressing a range of neurological conditions.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CTEP, Inhibitor, inhibit, Metabotropic glutamate receptors, mGluR5 inhibitor, mGluR5, mGluR, RO 4956371, RO4956371, RO-4956371

Compound Identifiers

PubChem CID

11646823