Fosmanogepix TFA
Fosmanogepix TFA (APX001 TFA) is an orally active APX001A (HY-18233) prodrug and antifungal agent. Fosmanogepix TFA is effective against Cryptococcus neoformans, Fluconazole (HY-B0101)-resistant C. auris. Fosmanogepix TFA is effective in the treatment of invasive pulmonary aspergillosis and pulmonary murine mucormycosis.
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- 화학식: C24H22F3N4O8P
- 분자량:582.42
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
Fosmanogepix (78-264 mg/kg; p.o.; once or twice daily; 3-7 days) TFA significantly increases the median survival time and 21-day survival rate of immunosuppressed mice with invasive pulmonary aspergillosis (IPA) infection, and reduces the pulmonary fungal burden by up to 7.64 log10 conidial equivalent/g[2].
Fosmanogepix (104-260 mg/kg; i.p.; three/two times daily; 7 days) TFA exerts protective effects against *Candida auris* invasive candidiasis in mouse models[3].
Fosmanogepix (52-104 mg/kg; p.o.; once daily; 7 days) TFA significantly improves the survival rate of neutropenic mice with pulmonary mucormycosis caused by Rhizopus arrhizus var. delemar 99-880[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (male; infected with 5.9 x 104 CFU *C. neoformans* strain H99 via lateral tail vein injection)[1]
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Dosage:390 mg/kg
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Administration:p.o.; three times daily; 7 days
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Result:Reduced brain fungal burden by 0.78 log10 CFU/g relative to untreated controls.
Reduced lung fungal burden by 1.50 log10 CFU/g relative to untreated controls.
Achieved statistically significant reduction in lung fungal burden relative to controls.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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분자량 582.42
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화학식 C24H22F3N4O8P
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Color White to off-white
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SMILES
N=C1C(C2=CC(CC3=CC=C(C=C3)COC4=NC=CC=C4)=NO2)=CC=CN1COP(O)(O)=O.O=C(O)C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 8.33 mg/mL (14.30 mM; ultrasonic and adjust pH to 4 with 1 M HCl; 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)
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Shaw KJ, et al. In Vitro and In Vivo Evaluation of APX001A/APX001 and Other Gwt1 Inhibitors against Cryptococcus. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00523-18. [Content Brief]
[2]. Gebremariam T, et al. APX001 Is Effective in the Treatment of Murine Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2019;63(2):e01713-18. Published 2019 Jan 29. [Content Brief]
[3]. Wiederhold NP, et al. Efficacy of Delayed Therapy with Fosmanogepix (APX001) in a Murine Model of Candida auris Invasive Candidiasis. Antimicrob Agents Chemother. 2019;63(11):e01120-19. Published 2019 Oct 22. [Content Brief]
[4]. Gebremariam T, et al. Fosmanogepix (APX001) Is Effective in the Treatment of Pulmonary Murine Mucormycosis Due to Rhizopus arrhizus. Antimicrob Agents Chemother. 2020;64(6):e00178-20. Published 2020 May 21. [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 | 1.7170 mL | 8.5849 mL | 17.1697 mL | 42.9244 mL |
| 5 mM | 0.3434 mL | 1.7170 mL | 3.4339 mL | 8.5849 mL | |
| 10 mM | 0.1717 mL | 0.8585 mL | 1.7170 mL | 4.2924 mL |
Fosmanogepix TFA Related Classifications
HY-119726B Related Classifications
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