(Rac)-Modipafant (UK-74505) 是一种口服的、选择性的、长效的不可逆血小板活化因子受体(PAFR)受体拮抗剂。(Rac)-Modipafant 预防严重登革热感染。
| 生物活性 | (Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversibleplatelet activating factor receptor (PAFR)antagonist. (Rac)-Modipafant prevents dengueinfection[1][2][3]. |
体内研究
(In Vivo) | (Rac)-Modipafant (UK-74505) (10 mg/kg; p.o.; twice a day until day 10) prevents Severe Dengue Infection[3].
(Rac)-Modipafant exhibits highly selective, time-dependent inhibition of PAF-induced aggregation of rabbit washed platelets (IC50=26.3 and 1.12 nM after 0.25 and 60 min preincubation, respectively)[4].
(Rac)-Modipafant (5-20 mg/kg; p.o.) dose-dependently inhibits the Zymosan -induced articular hyperalgesia[5].
| Animal Model: | 8- to 10-week-old BALB/c mice (DEN-2 strain infected)[3] | | Dosage: | 10 mg/kg | | Administration: | P.o.; twice a day (started on days 0, 3, 5, or 7) until day 10 | | Result: | Decreased by approximately 50% the lethality associated with DEN-2 infection. |
| Animal Model: | Male BALB/C (8- to 10- week-old) wild-type mice[5] | | Dosage: | 5, 10 and 20 mg/kg | | Administration: | P.o. | | Result: | Dose-dependently inhibited the Zymosan -induced articular hyperalgesia. |
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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(82.63 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.6526 mL | 8.2632 mL | 16.5265 mL | | 5 mM | 0.3305 mL | 1.6526 mL | 3.3053 mL | | 10 mM | 0.1653 mL | 0.8263 mL | 1.6526 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 (4.13 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.13 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。 *以上所有助溶剂都可在本网站选购。
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