DSM265

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DSM265 是一种长效的恶性疟原虫二氢乳清酸脱氢酶 PfDHODH 抑制剂，其 IC50 值为 8.9 nM。DSM265 还可以抑制 Pf3D7 的生长，其 EC50 值为 4.3 nM。

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM.

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DSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD-scid IL-2Rγnull (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose (ED90) of 3 mg/kg per day (1.5 mg/kg twice daily). The maximum rate of parasite killing occurred at and above a dose of 13 mg/kg per day (6.4 mg/kg twice daily). DSM265 has moderate terminal elimination half-life (t1/2) of 2-4 hours for mice (0.5 to 75 mg/kg, oral) .Animal Model:NOD-scid IL-2Rγnull (NSG) mice (23-36 g)Dosage:0.5 to 75 mg/kg Administration:Oral administration; twice daily; for 4 days Result:Had potent antimalarial activity with 90% effective dose (ED90) of 3 mg/kg per day (1.5 mg/kg twice daily).

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Metabolic Enzyme/Protease

Dehydrogenase

Dehydrogenase | Parasite

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1282041-94-4

415.33

C14H12F7N5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (120.39 mM; 超声助溶 )Ethanol 中的溶解度 : 11.11 mg/mL (26.75 mM; 超声助溶)

Cc1cc(Nc2ccc(cc2)S(F)(F)(F)(F)F)n2nc(nc2n1)C(C)(F)F

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(-20℃)

With Ice Pack

≥ 2 years