2. Anti-infection
  3. Parasite
  4. AWZ1066S

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) .

For research use only. We do not sell to patients.

AWZ1066S Chemical Structure

AWZ1066S Chemical Structure

CAS No. : 2239272-16-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 180 In-stock
25 mg USD 290 In-stock
50 mg USD 420 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

AWZ1066S Related Antibodies

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

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

AWZ1066S Related Antibodies
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

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
Molecular Weight

404.39

Formula

C19H19F3N6O
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4729 mL 12.3643 mL 24.7286 mL
5 mM 0.4946 mL 2.4729 mL 4.9457 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.64%

COA (255 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AWZ1066S2239272-16-1Parasiteoralanti-WolbachiaCYP2C9CYP3A4tropical diseasesOnchocerciasis (river blindness)lymphatic filariasis (elephantiasis)Inhibitorinhibitorinhibit

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