AWZ1066S

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

AWZ1066S 是一种高度特异性的抗沃尔巴克氏体候选化合物，用于短期治疗丝虫病（细胞测定中 EC50：2.5 nM）。

AWZ1066S is a highly specific anti-Wolbachia drug candidate for the short-course treatment of filariasis (EC50: 2.5 nM in cell assay).

AWZ1066S has anti-Wolbachia activity with EC50 value of 121 nM.AWZ1066S has a weak CYP2C9 inhibitory activity with an IC50 value of 9.7 μM and has a weak CYP3A4 induced activity with an IC50 value of 37 uM, but does not show any time-dependent inhibition across five majorhuman CYP450 isoforms (CYP1A, CYP2C9, CYP2C19, CYP2D6, CYP3A).

AWZ1066S (oral; 50, 100 mg/kg; bid; for 7 days) has high anti-Wolbachia efficacy.AWZ1066S (i.v or p.o; 5, 10, 85, 90 242 mg/kg) can oral delivery and has good aqueous solubility and metabolic stability.Mouse PK profiles of AWZ1066S and its mesylate salt in BALB/c mice (n=3).Animal Model:SCID mice Dosage:50, 100 mg/kg Administration:oral, bid, for 7 days Result:Showed good anti-Wolbachia effects.Animal Model:BALB/c SCID mice Dosage:5, 10, 85, 90 242 mg/kg Administration:i.v or p.o Result:Showed good aqueous solubility and metabolic stability.

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Microbiology/Virology

Parasite

Parasite

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2239272-16-1

404.39

C19H19F3N6O

>98% (HPLC)

DMSO:120 mg/mL (296.74 mM; Need ultrasonic)

C[C@@H](COCC1)N1c1nc2ncccc2c(NCc2cccnc2C(F)(F)F)n1

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(-20℃)

With Ice Pack

≥ 2 years