S88418 |
KDU691 |
| 源叶(MedMol) | 98% |
- 产品描述： KDU691 is a PI4K inhibitor.
- 靶点： Parasite;PI4K
- 体内研究：
KDU691 was evaluated for in vivo activity in rhesus macaques infected with P. cynomolgi sporozoites.?The prophylactically treated monkeys failed to become blood smear positive, while untreated control animals showed normal parasitemia development (primary parasitemia at day 8.9 p.i., with the first relapse within a month).?Thus, 5-day oral treatment with 20 mg/kg of KDU691 shortly after infection eradicated all liver-stage parasites, including hypnozoites.
- 动物实验： Sporozoites were harvested from P. cynomolgi-infected mosquitoes, washed with phosphate-buffered saline (PBS), and diluted to 100,000 sporozoites (spz)/ml in PBS. One-milliliter aliquots of sporozoites were prepared and injected into monkeys via intravenous injection. During treatment, monkeys were weighed daily and received the compound via gavage, followed by gastric feeding. Monkeys in the prophylaxis groups were treated 20 min after the i.v. sporozoite injection. The other monkeys were treated when all the monkeys in the experiment (except those in the prophylaxis group) were blood-stage patent (at day 11 p.i.). To kill the blood-stage parasites, all monkeys received a 5-day treatment of 7.5 mg/kg of body weight of chloroquine (CQ), during compound dosing. KDU691 was formulated in 0.5% methylcellulose and 0.5% Tween 80 in water. LMV599 was formulated as a solid dispersion in a solution containing 5.6% (wt/wt) Tween 80 44.4% hydroxypropyl methylcellulose (HPMC) E3 38.9% Soluplus 11.1% vitamin E d-alphatoco
- 参考文献：
1. Zeeman A M , Lakshminarayana S B , Werff N V D , et al. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites[J]. Antimicrobial Agents & Chemotherapy, 2016, 60(5):AAC.03080-15.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.382 ml 11.909 ml 23.817 ml 5 mM 0.476 ml 2.382 ml 4.763 ml 10 mM 0.238 ml 1.191 ml 2.382 ml 50 mM 0.048 ml 0.238 ml 0.476 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
