PC786 is an inhaled respiratory syncytial virus (RSV) L protein polymerase inhibitor. PC786 demonstrates potent antiviral activity against RSV-A (IC50 <0.09 to 0.71 nM) and RSV-B (IC50, 1.3 to 50.6 nM).
IC50&Target
RSV-A
0.09-0.71 nM (IC50)
RSV-B
1.3-50.6 nM (IC50)
体外研究
PC786 demonstrates a potent and selective antiviral activity against laboratory-adapted or clinical isolates of RSV-A (IC50<0.09 to 0.71 nM) and RSV-B (IC50, 1.3 to 50.6 nM), which are determined by inhibition of cytopathic effects in HEp-2 cells without causing detectable cytotoxicity. PC786 inhibits RSV A2 activity, exhibiting an IC50 and IC90 of 0.50±0.0014 nM and 0.63±0.035 nM, respectively. PC786 inhibits RSV B WST activity, exhibiting an IC50 and IC90 of 27.3±0.77 nM and 57.1±3.87 nM, respectively. PC786 exhibits potent inhibition of cytopathic effect (CPE) induced by known RSV A clinical isolates (IC50, 0.14 to 3.2 nM). PC786 also exhibits potent inhibition of CPE induced by various low-passage-number clinical isolates of RSV A (IC50, 0.42 nM [median]) and RSV B (IC50, 17.5 nM [median]).
体内研究
Once-daily treatment with PC786, on days-1 to 3, by either intratracheal (i.t.) or intranasal (i.n.) administration, is found to inhibit viral loads in the lungs of RSV A2-infected BALB/c mice. The viral load is below the level of detection when the drug is given at 2 mg/mL (40 μg/mouse [approximately 1.6 mg/kg of body weight] for i.t. treatment, or 80 μg/mouse [approximately 3.2 mg/kg] for i.n. treatment).
分子式
C41H38FN5O4S
分子量
715.83
CAS号
1902114-15-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-80°C, stored under nitrogen
溶解性数据
In Vitro:
DMSO : 130 mg/mL (181.61 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.3970 mL
6.9849 mL
13.9698 mL
5 mM
0.2794 mL
1.3970 mL
2.7940 mL
10 mM
0.1397 mL
0.6985 mL
1.3970 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°C, 6 months (stored under nitrogen)。-80°C 储存时,请在 6 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: