Pafuramidine (DB289) 是一种具有口服活性的 Furamidine (HY-110137A) 前药。Pafuramidine 是一种有效的抗寄生虫剂，可用于锥虫病、肺囊虫肺炎和疟疾的研究。
| 生物活性 | Pafuramidine (DB289) is an orally active prodrug ofFuramidine(HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis,Pneumocystispneumonia and malaria[1][2][3]. |
| IC50& Target[1][3] | Trypanosoma | Plasmodium falciparum sporozoites |
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体内研究
(In Vivo) | Pafuramidine (1-10 mg/kg; p.o.; for 5 or 10 days) cures some trypanosomes-infected monkeys[1].
Pafuramidine (2.5-100 mg/kg; p.o.; for 4 or 5 days) cures someTrypanosoma brucei-infected mice[5].
| Animal Model: | Vervet monkeys (infected by intravenous injection of 104trypanosomes)[1] | | Dosage: | 1, 3, and 10 mg/kg (group 1/2/3); 10 mg/kg (group 4/5) | | Administration: | p.o.; 5 consecutive days for group 1/2/3 (started on the 7th day postinfection); 10 days for group 4 (started on the 14th day postinfection); 10 days for group 5 (started on the 28th day postinfection). Post-treatment monitoring was maintained for a period of 180 days. | | Result: | Cured all three monkeys in group 3 at 10 mg/kg, and did not recur during the monitoring period.
All three monkeys in group 4 became aparasitemic by day 5 of dosing, but only two of three monkeys remained free of blood parasites until 180 days post-treatment monitoring.
All three monkeys in group 5 became aparasitemic by day 4 of dosing, but only two of three of monkeys remained free of blood trypanosomes by the end of the 180 days of post-treatment monitoring. |
| Animal Model: | Female NMRI mice (infected intraperitoneally with 2 × 104STIB900 bloodstream forms)[5] | | Dosage: | 2.5, 5, 25 and 50 mg/kg | | Administration: | p.o.; for 4 days (started on the 4th day postinfection) | | Result: | Cured all four mice at 25 and 50 mg/kg. |
| Animal Model: | Female NMRI mice (infected intraperitoneally with 2 × 104GVR35 bloodstream forms)[5] | | Dosage: | 25, 50 and 100 mg/kg | | Administration: | p.o.; for 5 days (started on the 21st day postinfection) | | Result: | Showed good CNS activity in the GVR35 CNS model, with 3/5 mice cured at 100 mg/kg. |
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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 : 33.33 mg/mL(91.47 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7442 mL | 13.7212 mL | 27.4424 mL | | 5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | | 10 mM | 0.2744 mL | 1.3721 mL | 2.7442 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 90%corn oil Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.86 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。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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