AWZ1066S

AWZ1066S is a highly potent, specific and orally active anti-Wolbachia agent with EC₅₀ value of 121 nM. AWZ1066S also is a weak CYP2C9 inhibitor and a weak CYP3A4 inducer with IC₅₀ values of 9.7 μM and 37 uM, respectively. AWZ1066S can be used for the research of tropical diseases such as Onchocerciasis (river blindness) and lymphatic filariasis (elephantiasis) ^[1]. IC50 & Target:EC50: 121 nM (anti-Wolbachia)^[1] In Vitro:AWZ1066S has anti-Wolbachia activity with EC₅₀ value of 121 nM^[1].
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)^[1]. In Vivo:AWZ1066S (oral; 50, 100 mg/kg; bid; for 7 days) has high anti-Wolbachia efficacy^[1].
AWZ1066S (i.v or p.o; 5, 10, 85, 90 242 mg/kg) can oral delivery and has good aqueous solubility and metabolic stability^[1].
Mouse PK profiles of AWZ1066S and its mesylate salt in BALB/c mice (n=3)

Dose(mg/kg)	Cmax(μg/mL)	tmax(hr)	t1/2(hr)	AUC0-24h(μg/mL*hr)	Vss(mL/kg)	CLtot(mL/hr/kg)	BA(%)
5IV	-	-	3.5	10.7	317.3	466.7	-
10PO	16.2	0.17	-	18.0	-	-	84
90PO	46.6	0.75	-	132.3	-	-	91
85PO	43.4	0.83	-	119.2	-	-	86
242PO	87.3	0.17	-	210.2	-	-	54