产品
编 号：F198134
分子式：C16H8ClFN4
分子量：310.71
分子式：C16H8ClFN4
分子量：310.71
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1644645-32-8
产品详情
生物活性：
HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pKi?and a pIC50 of 9.3 and 9.2, respectively. HTL14242 can be used for the research of parkinson’s disease.
体内研究：
HTL14242 (oral administration; 1, 3, or 10 mg/kg; sacrificed 1 h postdose) emonstrates an excellent, dose-dependent occupancy of mGlu5?receptors from an oral dose, with an estimated ED50?of 0.3 mg/kg. HTL14242 (oral administration; 1 mg/ml) exhibits an oral PK Profile, the t1/2,AUCinf?and F% are 6.5 hours, 3946 ng/h/mL and 80%, respectively in dog.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.
体外研究：
HTL14242 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 TC50?is >90 μM.
HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pKi?and a pIC50 of 9.3 and 9.2, respectively. HTL14242 can be used for the research of parkinson’s disease.
体内研究：
HTL14242 (oral administration; 1, 3, or 10 mg/kg; sacrificed 1 h postdose) emonstrates an excellent, dose-dependent occupancy of mGlu5?receptors from an oral dose, with an estimated ED50?of 0.3 mg/kg. HTL14242 (oral administration; 1 mg/ml) exhibits an oral PK Profile, the t1/2,AUCinf?and F% are 6.5 hours, 3946 ng/h/mL and 80%, respectively in dog.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.
体外研究：
HTL14242 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 TC50?is >90 μM.
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