Opelconazole
Based on 1 publication(s) in Google Scholar
Opelconazole (PC945), a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. Opelconazole is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively.
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- Pureza: 98.41%
- No. CAS: 1931946-73-4
- Fòrmula: C38H37F3N6O3
- Peso molecular:682.73
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Opelconazole
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Actividad biológica
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fungal |
CYP51A 0.23 μM (IC50) |
CYP51B 0.22 μM (IC50) |
Opelconazole (PC945) is a triazole antifungal designed for administration via inhalation[1].
Opelconazole (PC945) exhibits the most potent antifungal activity on azole-susceptible strain NCPF2010 with the MIC value of 0.063 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Specific-pathogen-free A/J mice (male, 5 weeks old, pulmonary Aspergillus infection)[1]
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Dosage:0.56, 2.8, 14 μg/mouse (intranasal application of 0.016-, 0.08-, and 0.4-mg/ml suspensions, respectively)
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Administration:Intranasal; daily for 7 days
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Result:Substantially inhibited the incidence of rolling behavior.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1931946-73-4
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Appearance Solid
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Peso molecular 682.73
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Fòrmula C38H37F3N6O3
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C(F)C=C1)C(C=C2)=CC=C2N3CCN(C4=CC=C(OC[C@@H]5CO[C@](C6=CC=C(F)C=C6F)(CN7N=CN=C7)C5)C(C)=C4)CC3
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Synonyms
PC945
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Microbiol Spectr
Multicenter surveillance of antifungal susceptibility of clinical Aspergillus isolates to conventional and novel antifungal agents in Taiwan, 2021-2023. [Abstract]2026 Apr 21:e0265925. PMID: 42012212
Solvente y solubilidad
DMSO : 100 mg/mL (146.47 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: 2.5 mg/mL (3.66 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (272 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
[1]. Colley T, et al. In Vitro and In Vivo Antifungal Profile of a Novel and Long-Acting Inhaled Azole, PC945, on Aspergillus fumigatus Infection. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02280-16. [Content Brief]
[2]. Colley T, et al. Antifungal synergy of a topical triazole, PC945, with a systemic triazole against respiratory Aspergillus fumigatus infection. Sci Rep. 2019 Jul 1;9(1):9482. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4647 mL | 7.3235 mL | 14.6471 mL | 36.6177 mL |
| 5 mM | 0.2929 mL | 1.4647 mL | 2.9294 mL | 7.3235 mL | |
| 10 mM | 0.1465 mL | 0.7324 mL | 1.4647 mL | 3.6618 mL | |
| 15 mM | 0.0976 mL | 0.4882 mL | 0.9765 mL | 2.4412 mL | |
| 20 mM | 0.0732 mL | 0.3662 mL | 0.7324 mL | 1.8309 mL | |
| 25 mM | 0.0586 mL | 0.2929 mL | 0.5859 mL | 1.4647 mL | |
| 30 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2206 mL | |
| 40 mM | 0.0366 mL | 0.1831 mL | 0.3662 mL | 0.9154 mL | |
| 50 mM | 0.0293 mL | 0.1465 mL | 0.2929 mL | 0.7324 mL | |
| 60 mM | 0.0244 mL | 0.1221 mL | 0.2441 mL | 0.6103 mL | |
| 80 mM | 0.0183 mL | 0.0915 mL | 0.1831 mL | 0.4577 mL | |
| 100 mM | 0.0146 mL | 0.0732 mL | 0.1465 mL | 0.3662 mL |
Opelconazole Related Classifications
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