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Home   »   Product Pathways  »  mGluR  »  CTEP

Products are for research use only. Not for human use. We do not sell to patients.

CS-0974 CTEP

(mGluR5 inhibitor)
Structure Price and Availability of    CTEP
United States
Size Price Stock
5mg $110 In-stock Inquiry
10mg $190 In-stock
50mg $700 In-stock
100mg $1200 In-stock
200 mg Get quote
500 mg Get quote
 Distributor In Japan:  フナコシ株式会社    電話番号:81-3-5684-1620   
Inquiry for price and availability only. Please place your order via our email or fax.
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  • Data Sheet
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CTEP  M.Wt:  391.77
CTEP  Formula: C19H13ClF3N3O
CTEP  Solubility: DMSO > 50 mg/mL Ethanol > 50 mg/mL
CTEP  Purity: >98%
CTEP  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 871362-31-1

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CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM. IC50 Value: 2.2 nM Target: mGluR5 in vivo: CTEP is a novel, potent, selective and orally bioavailable allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5. CTEP binds mGlu5 with low nanomolar affinity and shows >1000-fold selectivity when tested against 103 targets, including all known mGlu receptors. In animal studies CTEP was found to have a high oral bioavailability and a long duration of action, lasting 18 hours after a single dose, giving it considerably improved properties over older mGluR5 antagonists such as MPEP and fenobam. in vivo: 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. 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.

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