Narlaprevir (SCH 900518) 是一种选择性的且有口服活性的NS3 protease抑制剂,Ki值为 6 nM,EC90值为 40 nM。Narlaprevir 还抑制丙型肝炎病毒 (HCV) 非结构蛋白3丝氨酸蛋白酶。Narlaprevir 可用于慢性丙型肝炎研究。Narlaprevir 也是SARS-CoV 3CLpro的抑制剂,IC50为 2.3 μM。
生物活性 | Narlaprevir (SCH 900518) is a selective and orally bioavailableNS3 proteaseinhibitor with aKivalue of 6 nM and anEC90value of 40 nM[1]. Narlaprevir also inhibits theHCVnonstructural protein 3 serine protease[2]. Narlaprevir is also aSARS-CoV3CLproinhibitor with anIC50of 2.3 μM[3]. |
IC50& Target | Ki: 6 nM (NS3 protease)[1] EC90: 40 nM (NS3 protease)[1] Ki: 7 nM (ketoamide)[2] EC90: 40 nM (replicon RNA)[2] |
体外研究 (In Vitro) | Narlaprevir (SCH 900518) potently inhibits ketoamide with a Kivalue of 7 nM[2]. Narlaprevir (SCH 900518) potently inhibits replicon RNA with an EC90value of 40 nM[2].
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体内研究 (In Vivo) | Pharmacokinetic Analysis Narlaprevir (SCH 900518) exhibits middle oral bioavailability (rat 46%, dog 29%, monkey 46 %) following oral administration (rat 10 mg/kg, dog 3 mg/kg, monkey 3 mg/kg )[1]. Narlaprevir (SCH 900518) exhibits moderate half-lives (rat 4.8 and dog 2 h) following intravenous administration (rat 4 and dog 1 mg/kg)[1].
Animal Model: | rats, dogs, monkeys[1] | Dosage: | Rat PO/IV 10/4 mg/kg; dog PO/IV 3/1 mg/kg; monkey PO 3 mg/kg | Administration: | Intravenous (i.v.) or oral gavage | Result: | T1/2s of 4.8 and 2 h for rats and dogs, respectively. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(70.63 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.4125 mL | 7.0625 mL | 14.1251 mL | 5 mM | 0.2825 mL | 1.4125 mL | 2.8250 mL | 10 mM | 0.1413 mL | 0.7063 mL | 1.4125 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.53 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.53 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.53 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.53 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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