| Identification | Back Directory | [Name]
AWZ1066S | [CAS]
2239272-16-1 | [Synonyms]
AWZ1066S
AWZ1066S;AWZ-1066S;AWZ 1066S
2-[(3S)-3-Methyl-4-morpholinyl]-N-[[2-(trifluoromethyl)-3-pyridinyl]methyl]pyrido[2,3-d]pyrimidin-4-amine
Pyrido[2,3-d]pyrimidin-4-amine, 2-[(3S)-3-methyl-4-morpholinyl]-N-[[2-(trifluoromethyl)-3-pyridinyl]methyl]- | [Molecular Formula]
C19H19F3N6O | [MDL Number]
MFCD31813769 | [MOL File]
2239272-16-1.mol | [Molecular Weight]
404.39 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis, with an EC50 of 2.5 nM in cell assay[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 |
| Animal Model: | SCID mice[1] | | Dosage: | 50, 100 mg/kg | | Administration: | oral, bid, for 7 days | | Result: | Showed good anti-Wolbachia effects. |
| Animal Model: | BALB/c SCID mice[1] | | Dosage: | 5, 10, 85, 90 242 mg/kg | | Administration: | i.v or p.o | | Result: | Showed good aqueous solubility and metabolic stability. |
| [References]
[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. |
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