Basic information Safety Supplier Related

AWZ1066S

Basic information Safety Supplier Related

AWZ1066S Basic information

Product Name:
AWZ1066S
Synonyms:
  • AWZ1066S
  • AWZ1066S;AWZ-1066S;AWZ 1066S
  • Pyrido[2,3-d]pyrimidin-4-amine, 2-[(3S)-3-methyl-4-morpholinyl]-N-[[2-(trifluoromethyl)-3-pyridinyl]methyl]-
  • 2-[(3S)-3-Methyl-4-morpholinyl]-N-[[2-(trifluoromethyl)-3-pyridinyl]methyl]pyrido[2,3-d]pyrimidin-4-amine
  • oral,Inhibitor,anti-Wolbachia,Onchocerciasis (river blindness),CYP3A4,AWZ1066S,Parasite,AWZ-1066S,CYP2C9,tropical diseases,inhibit,lymphatic filariasis (elephantiasis)
  • 2-[(3S)-3-methylmorpholin-4-yl]-N-{[2-(trifluoromethyl)pyridin-3-yl]methyl}pyrido[2,3-d]pyrimidin-4-amine
  • AWZ1066S, 10 mM in DMSO
CAS:
2239272-16-1
MF:
C19H19F3N6O
MW:
404.39
Mol File:
2239272-16-1.mol
More
Less

AWZ1066S Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMSO : 125 mg/mL (309.11 mM; Need ultrasonic)
form 
Solid
color 
White to off-white
More
Less

AWZ1066S Usage And Synthesis

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--3.510.7317.3466.7-
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[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.

AWZ1066SSupplier

Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Email
2853530910@QQ.com
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Email
Sales@ATKchemical.com
Shanghai SuperLan Chemcial Technique Centre
Tel
0-2022843681 15618226720
Email
chaolaichem@foxmail.com
Chuzhou KeMail Chemical Technology Co., Ltd
Tel
0550-5196001 15000891977
Email
wj520wjxby@126.com