产品
编 号：F281155
分子式：C19H19F3N6O
分子量：404.39
分子式：C19H19F3N6O
分子量：404.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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询价
5mg
询价
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10mg
询价
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25mg
询价
询价
50mg
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结构图
CAS No: 2239272-16-1
产品详情
生物活性：
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) .
体内研究：
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)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--3.510.7317.3466.7-
10PO16.20.17-18.0--84
90PO46.60.75-132.3--91
85PO43.4 0.83-119.2--86
242PO87.3 0.17-210.2--54
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.
体外研究：
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 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) .
体内研究：
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)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--3.510.7317.3466.7-
10PO16.20.17-18.0--84
90PO46.60.75-132.3--91
85PO43.4 0.83-119.2--86
242PO87.3 0.17-210.2--54
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.
体外研究：
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).
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