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Purity: ≥98%
CTEP (also called RO4956371; RO 4956371; RO-4956371) is a long-acting and orally bioavailable allosteric antagonist of metabotropic glutamate receptor 5 (mGlu5) receptor with important biological activity. It inhibits mGlu5 with an IC50 of 2.2 nM and exhibits >1000-fold selectivity for mGlu5 over other mGlu receptors.
| ln Vitro |
In HEK293 cells that are stable in the expression of human mGlu5, CTEP (RO 4956371) 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 that are stable in expressing human mGlu5, CTEP (RO 4956371) inhibits the constitutive activity of human mGlu5 by roughly 50% at an IC50 of 40.1 nM[1].
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| ln Vivo |
In mice treated for anxiety, CTEP (RO 4956371) is notably effective at doses of 0.1 mg/kg and 0.3 mg/kg. In the Vogel conflict drinking test, CTEP (RO 4956371) has no impact at lower dosages but considerably lengthens drinking times at 0.3 and 1.0 mg/kg. The B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice, while the half-life of CTEP (RO 4956371) (oral) is 18 hours. After being given to adult C57BL/6 mice in single oral dosages of 4.5 and 8.7 mg/kg as a microsuspension in a saline/Tween vehicle, CTEP (RO 4956371) is quickly absorbed and reaches nearly maximal exposure in about 30 minutes. The minimum CTEP (RO 4956371) brain exposure in adult mice administered chronically at a dose of 2 mg/kg po every 48 hours for two months is 240 ng/g. CTEP (RO 4956371) completely displaces [3H]ABP688 in mouse brain regions where mGlu5 expression is known, and dosages that result in an average compound concentration of 77.5 ng/g when evaluated in whole brain homogenate can accomplish 50% displacement[1]. In mice, continuous mGlu5 occupancy is achieved every 48 hours with CTEP (RO 4956371; 2 mg/kg, po bid). The Fmr1 knockout mouse's heightened hippocampus long-term depression, excessive protein synthesis, and audiogenic seizures are corrected by CTEP (RO 4956371) (2 mg/kg, po) treatment[2].
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| References |
[1]. Lindemann L, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86.
[2]. Michalon A, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 2012 Apr 12;74(1):49-56 |
| Molecular Formula |
C19H13CLF3N3O
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| Molecular Weight |
391.77
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| CAS # |
871362-31-1
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| Related CAS # |
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| SMILES |
FC(F)(F)OC1=CC=C(N2C(C)=C(C#CC3=CC(Cl)=NC=C3)N=C2C)C=C1
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| Chemical Name |
2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
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| Synonyms |
RO-4956371; CTEP; RO4956371; RO 4956371;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5525 mL | 12.7626 mL | 25.5252 mL | |
| 5 mM | 0.5105 mL | 2.5525 mL | 5.1050 mL | |
| 10 mM | 0.2553 mL | 1.2763 mL | 2.5525 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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