CTEP ( RO4956371; RO-4956371; RO 4956371; CTEP )

Catalog No. M17635 CAS No. 871362-31-1

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Product Name

CTEP
Note

Research use only, not for human use.
Brief Description

CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.
Description

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.
Synonyms

RO4956371; RO-4956371; RO 4956371; CTEP
Pathway

Endocrinology/Hormones
Target

5-HT Receptor
Recptor

mGluR5
Research Area

Neurological Disease
Indication

——

CAS Number

871362-31-1
Formula Weight

391.77
Molecular Formula

C19H13ClF3N3O
Purity

98%
Solubility

DMSO : ≥ 100 mg/mL. 255.25 mM; H2O : < 0.1 mg/mL
SMILES

CC1=NC(C#CC2=CC=NC(Cl)=C2)=C(C)N1C1=CC=C(OC(F)(F)F)C=C1
Chemical Name

2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine

1. Lindemann L, et al. J Pharmacol Exp Ther, 2011, 339(2), 474-486.

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