CTEP, also known as RO4956371, is a potent, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM. CTEP binds mGlu5 with low nanomolar affinity and shows >1000-fold selectivity when tested against 103 targets, including all known mGlu receptors. CTEP penetrates the brain with a brain/plasma ratio of 2.6 and displaces the tracer ABP688 in vivo in mice from brain regions expressing mGlu5 with an average ED(50) equivalent to a drug concentration of 77.5 ng/g in brain tissue.
CAS Number: 871362-31-1
Molecular Weight: 391.77
Chemical Name: 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
CTEP was used at 0.03-0.1 µM final concentration in vitro and in cellular assays.
CTEP was orally dosed to mice at single 0.1-1.0 mg/kg, or with a dose of 2 mg/kg orally every 48 h for 2 months. CTEP was orally dose at 2 mg/kg BID achieves uninterrupted mGlu5 occupancy per 48 hours in mice.
- Lindemann L, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. (2011) J Pharmacol Exp Ther. 339(2):474-86.
- Michalon A, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. (2012) Neuron. 74(1):49-56.
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