产品
编 号：F430487
分子式：C22H19ClN6
分子量：402.88
分子式：C22H19ClN6
分子量：402.88
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 700361-47-3
产品详情
生物活性：
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV.
体内研究：
R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels.R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUCinf) amounts to 3.1 μg h/mL (4 mg/kg) in rat, 8.7 μg h/mL (1.25 mg/kg) in dog, 1.4 μg h/mL (1.25 mg/ kg) in monkey, and 44 μg h/mL (1.25 mg/kg) in rabbit.R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog.
体外研究：
R278474 对野生型 HIV-1 具有活性 (EC50=0.4 nM) 和所有测试的单突变体和双突变体 (EC50=0.1-2.0 nM)。R278474 (10-5000 nM; 30 d) 在 30 天内未观察到 1 μM 野生型 HIV-1 突破的迹象。R278474 在 50% 抑制浓度 (EC50) 小于 1 nM 时抑制 81% 的临床分离株（约 1200 种重组临床分离株），在 EC50 小于 10 nM 时则抑制 94%。TMC278 对野生型 HIV-1 M 组分离株 (0.07-1.01 nM) 显示亚纳摩尔的 EC50。
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV.
体内研究：
R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels.R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUCinf) amounts to 3.1 μg h/mL (4 mg/kg) in rat, 8.7 μg h/mL (1.25 mg/kg) in dog, 1.4 μg h/mL (1.25 mg/ kg) in monkey, and 44 μg h/mL (1.25 mg/kg) in rabbit.R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog.
体外研究：
R278474 对野生型 HIV-1 具有活性 (EC50=0.4 nM) 和所有测试的单突变体和双突变体 (EC50=0.1-2.0 nM)。R278474 (10-5000 nM; 30 d) 在 30 天内未观察到 1 μM 野生型 HIV-1 突破的迹象。R278474 在 50% 抑制浓度 (EC50) 小于 1 nM 时抑制 81% 的临床分离株（约 1200 种重组临床分离株），在 EC50 小于 10 nM 时则抑制 94%。TMC278 对野生型 HIV-1 M 组分离株 (0.07-1.01 nM) 显示亚纳摩尔的 EC50。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备