AWZ1066S

Product Name: AWZ1066S
CAS No.: 2239272-16-1
Chemical Name: AWZ1066S
Synonyms: AWZ1066S;AWZ1066S, 10 mM in DMSO;AWZ1066S;AWZ-1066S;AWZ 1066S;2-[(3S)-3-methylmorpholin-4-yl]-N-{[2-(trifluoromethyl)pyridin-3-yl]methyl}pyrido[2,3-d]pyrimidin-4-amine;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]-;oral,Inhibitor,anti-Wolbachia,Onchocerciasis (river blindness),CYP3A4,AWZ1066S,Parasite,AWZ-1066S,CYP2C9,tropical diseases,inhibit,lymphatic filariasis (elephantiasis)
CBNumber: CB74857313
Molecular Formula: C19H19F3N6O
Formula Weight: 404.39
MOL File: 2239272-16-1.mol

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AWZ1066S Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0084989
Product name: AWZ1066S
Purity: 98.65%
Packaging: 5mg
Price: $205
Updated: 2021/12/16

ChemScene

Product number: CS-0084989
Product name: AWZ1066S
Purity: 98.65%
Packaging: 10mg
Price: $350
Updated: 2021/12/16

ChemScene

Product number: CS-0084989
Product name: AWZ1066S
Purity: 98.65%
Packaging: 50mg
Price: $850
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb573421
Product name: AWZ1066S
Purity: >98%
Packaging: 50mg
Price: $1283.5
Updated: 2021/12/16

ChemScene

Product number: CS-0084989
Product name: AWZ1066S
Purity: 98.65%
Packaging: 100mg
Price: $1450
Updated: 2021/12/16

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AWZ1066S Chemical Properties,Usage,Production

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)	C_max(μg/mL)	t_max(hr)	t_1/2(hr)	AUC_0-24h(μg/mL*hr)	V_ss(mL/kg)	CL_tot(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.

AWZ1066S Preparation Products And Raw materials

Raw materials

Preparation Products

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AWZ1066S Suppliers

China 40 United States 3 Global 43

Shanghai Lollane Biological Technology Co.,Ltd.

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2239272-16-1, AWZ1066SRelated Search:

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

2239272-16-1

239272-16-1