| Bioactivity | 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]. | ||||||||||||
| Target | EC50: 121 nM (anti-Wolbachia) | ||||||||||||
| Invitro | 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) | ||||||||||||
| Name | AWZ1066S | ||||||||||||
| CAS | 2239272-16-1 | ||||||||||||
| Formula | C19H19F3N6O | ||||||||||||
| Molar Mass | 404.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Hong WD, et al. AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. Proc Natl Acad Sci U S A. 2019 Jan 22;116(4):1414-1419. |
AWZ1066S
CAS: 2239272-16-1 F: C19H19F3N6O W: 404.39
AWZ1066S is a highly potent, specific and orally active anti-Wolbachia agent with EC50 value of 121 nM. AWZ1066S also is
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