AWZ1066S
Based on 1 Customer Validation
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) .
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.39%
- No. CAS: 2239272-16-1
- Fòrmula: C19H19F3N6O
- Peso molecular:404.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
EC50: 121 nM (anti-Wolbachia)[1]
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 (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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2239272-16-1
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Appearance Solid
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Peso molecular 404.39
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Fòrmula C19H19F3N6O
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Color White to off-white
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SMILES
C[C@@H](COCC1)N1C2=NC3=C(C=CC=N3)C(NCC4=CC=CN=C4C(F)(F)F)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (291 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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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