Art. -Nr.: HY-114415

AWZ1066S

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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) .

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.39%
CAS. Nr.: 2239272-16-1
Formel: C₁₉H₁₉F₃N₆O
Molecular Weight:404.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AWZ1066S Chemical Structure

CAS. Nr.: 2239272-16-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 121 nM (anti-Wolbachia)^[1]

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In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2239272-16-1
Appearance Solid
Molecular Weight 404.39
Formel C₁₉H₁₉F₃N₆O
Color White to off-white
SMILES

C[C@@H](COCC1)N1C2=NC3=C(C=CC=N3)C(NCC4=CC=CN=C4C(F)(F)F)=N2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (309.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4729 mL

12.3643 mL

24.7286 mL

5 mM

0.4946 mL

2.4729 mL

4.9457 mL

10 mM

0.2473 mL

1.2364 mL

2.4729 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (291 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4729 mL	12.3643 mL	24.7286 mL	61.8215 mL
	5 mM	0.4946 mL	2.4729 mL	4.9457 mL	12.3643 mL
	10 mM	0.2473 mL	1.2364 mL	2.4729 mL	6.1822 mL
	15 mM	0.1649 mL	0.8243 mL	1.6486 mL	4.1214 mL
	20 mM	0.1236 mL	0.6182 mL	1.2364 mL	3.0911 mL
	25 mM	0.0989 mL	0.4946 mL	0.9891 mL	2.4729 mL
	30 mM	0.0824 mL	0.4121 mL	0.8243 mL	2.0607 mL
	40 mM	0.0618 mL	0.3091 mL	0.6182 mL	1.5455 mL
	50 mM	0.0495 mL	0.2473 mL	0.4946 mL	1.2364 mL
	60 mM	0.0412 mL	0.2061 mL	0.4121 mL	1.0304 mL
	80 mM	0.0309 mL	0.1546 mL	0.3091 mL	0.7728 mL
	100 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6182 mL

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AWZ1066S

Anti-Infection Compound Library

Clinical Compound Library

Orally Active Compound Library

Antiparasitic Compound library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AWZ1066S

Anti-Infection Compound Library

Clinical Compound Library

Orally Active Compound Library

Antiparasitic Compound library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AWZ1066S Related Classifications

HY-114415 Related Classifications