HTL14242 (C09-1138-549)

HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pK i and a pIC 50 of 9.3 and 9.2, respectively HTL14242 can be used for the research of parkinson’s disease .In VitroHTL14242 is stable in rat plasma, inactive at the hERG ion-channel, and has a clean profile in vitro assays of cytotoxicity in HepG2 cells, the TC 50 is >90 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoHTL14242 (oral administration; 1, 3, or 10 mg/kg; sacrificed 1 h postdose) emonstrates an excellent, dose-dependent occupancy of mGlu 5 receptors from an oral dose, with an estimated ED 50 of 0.3 mg/kg . HTL14242 (oral administration; 1 mg/ml) exhibits an oral PK Profile, the t 1/2 , AUC inf and F% are 6.5 hours, 3946 ng/h/mL and 80%, respectively in dog . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Dog (PK study) Dosage: 3, 10 and 30 mg/kg Administration: Oral administration; single dose Result: Had a good PK characteristics in dogs.IC50& Target:mGlu 5. Specification: 10mM in DMSO Molecular Formula: C16H8ClFN4 Molecular Weight: 310.71