Name: CTEP (RO4956371)
Price: 280.00 USD

- Overview
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    Background
    
    CTEP is a potent, long-acting, and orally bioavailable inhibitor of metabotropic glutamate receptor 5 (mGlu5) with IC50 value of 11.4nM [1].
    CTEP is a negative allosteric modulator of mGlu5 and has inverse agonist activity. In the in vitro binding assay, CTEP binds to human, mouse and rat mGlu5 with Kd values of 1.7nM, 1.8nM and 1.5 nM, respectively. In HEK293 cells expressing mGlu5, CTEP inhibits quisqualate-induced Ca2+ mobilization and inositol phosphate accumulation with IC50 value of 11.4nM and 6.4nM, respectively. In addition, it shows an IC50 value of 40.1nM in the IP accumulation assay, demonstrating its inverse agonist activity. CTEP is proved to be a highly selective inhibitor of mGlu5. It shows no significant activity against mGlu1, mGlu2, mGlu3, mGlu4, mGlu6, mGlu7 or mGlu8 at concentration up to 10μM [1].
    In the in vivo Vogel conflict drinking test, CTEP markedly increases drinking time at doses of 0.3mg/kg. In adult C57BL/6 mice brain, CTEP displaces the mGlu5 antagonist ABP688 in the regions expressing mGlu5 by 50% at dose of 77.5 ng/g [1].
    
    [1] Lindemann L, Jaeschke G, Michalon A, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. Journal of Pharmacology and Experimental Therapeutics, 2011, 339(2): 474-486.
- Properties
  - Alternative Name
    
    2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
    
    CAS Number
    
    871362-31-1
    
    Molecular Formula
    
    C19H13ClF3N3O
    
    Molecular Weight
    
    391.77
    
    Appearance
    
    A solid
    
    Purity
    
    98.27%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥19.6 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Choi WM, Kim HH, et al. "Glutamate Signaling in Hepatic Stellate Cells Drives Alcoholic Steatosis." Cell Metab. 2019 Aug 20. pii: S1550-4131(19)30430-9. PMID:31474565
    2. Sun Y, Lipton JO, et al. "Direct current stimulation induces mGluR5-dependent neocortical plasticity." Ann Neurol. 2016 Aug;80(2):233-46. PMID:27315032

CTEP (RO4956371)

CTEP (RO4956371)

Background

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