CTEP

Research use only, not for human use.

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.

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.

RO4956371; RO-4956371; RO 4956371; CTEP

Endocrinology/Hormones

5-HT Receptor

mGluR5

Neurological Disease

——

871362-31-1

391.77

C19H13ClF3N3O

98%

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

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

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

(-20℃)

With Ice Pack

≥ 2 years