Olorofim
Based on 1 Customer Validation
Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp..
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- Pureté: 99.38%
- CAS No.: 1928707-56-5
- Formule: C28H27FN6O2
- Masse moléculaire:498.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Dihydroorotate dehydrogenase[1]
Olorofim (0.1 μg/mL, 24-48 h) inhibits the spores germination and mycelium growth, exhibits antifungal activity against Aspergillus spp.[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:Aspergillus-infected mouse models[3]
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Dosage:15 mg/kg
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Administration:ip, every 8 hours for 9 days
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Result:Reduced granulomas and fungal hyphae in the lungs.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1928707-56-5
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Appearance Solid
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Masse moléculaire 498.55
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Formule C28H27FN6O2
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Color Light yellow to green yellow
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SMILES
O=C(NC1=CC=C(N2CCN(C3=NC=C(F)C=N3)CC2)C=C1)C(C4=C(C5=CC=CC=C5)C=C(C)N4C)=O
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Synonyms
F901318
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (200.58 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.
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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Lackner M, et al. Dihydroorotate dehydrogenase inhibitor olorofim exhibits promising activity against all clinically relevant species within Aspergillus section Terrei. J Antimicrob Chemother. 2018 Nov 1;73(11):3068-3073. [Content Brief]
[2]. du Pré S, et al., Effect of the Novel Antifungal Drug F901318 (Olorofim) on Growth and Viability of Aspergillus fumigatus. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00231-18. [Content Brief]
[3]. Seyedmousavi S, et al., Efficacy of Olorofim (F901318) against Aspergillus fumigatus, A. nidulans, and A. tanneri in Murine Models of Profound Neutropenia and Chronic Granulomatous Disease. Antimicrob Agents Chemother. 2019 May 24;63(6):e00129-19. [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 |
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| DMSO | 1 mM | 2.0058 mL | 10.0291 mL | 20.0582 mL | 50.1454 mL |
| 5 mM | 0.4012 mL | 2.0058 mL | 4.0116 mL | 10.0291 mL | |
| 10 mM | 0.2006 mL | 1.0029 mL | 2.0058 mL | 5.0145 mL | |
| 15 mM | 0.1337 mL | 0.6686 mL | 1.3372 mL | 3.3430 mL | |
| 20 mM | 0.1003 mL | 0.5015 mL | 1.0029 mL | 2.5073 mL | |
| 25 mM | 0.0802 mL | 0.4012 mL | 0.8023 mL | 2.0058 mL | |
| 30 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL | 1.6715 mL | |
| 40 mM | 0.0501 mL | 0.2507 mL | 0.5015 mL | 1.2536 mL | |
| 50 mM | 0.0401 mL | 0.2006 mL | 0.4012 mL | 1.0029 mL | |
| 60 mM | 0.0334 mL | 0.1672 mL | 0.3343 mL | 0.8358 mL | |
| 80 mM | 0.0251 mL | 0.1254 mL | 0.2507 mL | 0.6268 mL | |
| 100 mM | 0.0201 mL | 0.1003 mL | 0.2006 mL | 0.5015 mL |
Olorofim Related Classifications
HY-104029 Related Classifications
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