KDU731,具有口服活性的C. parvumPI4K抑制剂,阻断体内外隐孢子虫感染,IC50值为 25 nM。KDU731 是研究隐孢子虫引起的腹泻的有望候选药物,具有广泛的安全性。
生物活性 | KDU731, an orally activeC. parvumPI4Kinhibitor with anIC50value of 25 nM, blocksCryptosporidiuminfectionin vitro and in vivo[1][2]. KDU731 is a promising drug candidate for the treatment of diarrhea caused byCryptosporidiumand meets a broad range of safety[2]. |
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体内研究 (In Vivo) | KDU731 (orally administration; 7 or 10mg/kg; 16 days) has potent activity againstCryptosporidiumin immunocompromised IFN-γ KO mice and dramatically reduces oocyst shedding[2]. KDU731 (orally administration; 5 mg/kg; every 12 hours for 7 days) is tolerated in all calves, and treated calves shed significantly fewer oocysts than vehicle treated calves in their stool[2].
Animal Model: | 6-8 week old C57BL/6 IFN-γ-knockout mice with 10,000 oocysts[1] | Dosage: | 7 or 10 mg/kg | Administration: | Orally administration; 7 or 10 mg/kg; 16 days | Result: | Resulted in significant reduction of oocyst shedding. |
Animal Model: | Neonatal calves with 5 x 107oocysts[1] | Dosage: | 5 mg/kg | Administration: | Orally administration; 5 mg/kg; every 12 hours for 7 days | Result: | Resulted in significant reduction of oocyst shedding in treated calves in their stool. |
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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 : 83.33 mg/mL(210.22 mM;Need ultrasonic) 配制储备液 1 mM | 2.5227 mL | 12.6135 mL | 25.2270 mL | 5 mM | 0.5045 mL | 2.5227 mL | 5.0454 mL | 10 mM | 0.2523 mL | 1.2614 mL | 2.5227 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。 |