Ibrexafungerp
Based on 1 publication(s) in Google Scholar
Ibrexafungerp (MK 3118) is an orally active β-1,3-glucan synthesis inhibitor, with potential antifungal activity. Ibrexafungerp can be used for research of Candida and Aspergillus infections.
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- Purity: 99.83%
- CAS No.: 1207753-03-4
- 화학식: C44H67N5O4
- 분자량:730.03
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ibrexafungerp
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Biological Activity
Ibrexafungerp leads to fungicidal activity against various Candida spp., with MIC of 0.5 µg/mL[2].
Ibrexafungerp is effective against C. albicans, C. krusei, C. parapsilosis with MICs of 0.06, 0.5, 0.25 µg/mL[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ibrexafungerp (p.o., mouse 1 mg/kg, rat 5 mg/kg and dog 5 mg/kg) exhibits oral bioavailability (mouse 51%, rat 45%, dog 35%)[3].
Ibrexafungerp (i.v., mouse 1 mg/kg, rat 5 mg/kg and dog 5 mg/kg) exhibits moderate half-lives (mouse 5.5, rat 8.7 and, dog 9.3 h) due to high plasma clearance (0.68, 0.44, and 0.45 L/h/kg respectively)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pig cutaneous infection model (C. auris)[3]
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Dosage:10 mg/kg
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Administration:Oral administration.
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Result:Reduced the severity of lesions and significantly reduced the C. auris fungal burden.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1207753-03-4
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Appearance Solid
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분자량 730.03
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화학식 C44H67N5O4
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Color White to off-white
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SMILES
C[C@@]12[C@@](CC3)([H])[C@@](C[C@](N4C(C5=CC=NC=C5)=NC=N4)([H])[C@@H]1OC[C@](C)(N)C(C)(C)C)(COC2)C([C@@]3([H])[C@]6(CC[C@]7(C)[C@H](C)C(C)C)C)=CC[C@]6([C@@H]7C(O)=O)C
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Synonyms
MK 3118; SCY-078
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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
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
용액&용해도
DMSO : 100 mg/mL (136.98 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 (3.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
순도&문서
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Data Sheet (279 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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Handling Instructions (2659 KB)
References
[1]. James M Apgar, et al. Ibrexafungerp: An orally active β-1,3-glucan synthesis inhibitor. Bioorg Med Chem Lett. 2021 Jan 15;32:127661. [Content Brief]
[2]. Mahmoud Ghannoum, et al. Ibrexafungerp: A Novel Oral Triterpenoid Antifungal in Development for the Treatment of Candida auris Infections. Antibiotics (Basel). 2020 Aug 25;9(9):539. [Content Brief]
[3]. Stephen A Wring, et al. Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis. Antimicrob Agents Chemother. 2017 Mar 24;61(4):e02068-16. [Content Brief]
[4]. Ghannoum M, et al. Efficacy of Ibrexafungerp (SCY-078) against Candida auris in an In Vivo Guinea Pig Cutaneous Infection Model. Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00854-20. [Content Brief]
[5]. Arendrup MC, et al. In Vitro Activity of Ibrexafungerp (SCY-078) against Candida auris Isolates as Determined by EUCAST Methodology and Comparison with Activity against C. albicans and C. glabrata and with the Activities of Six Comparator Agents. Antimicrob Agents Chemother. 2020 Feb 21;64(3):e02136-19. [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 | 1.3698 mL | 6.8490 mL | 13.6981 mL | 34.2452 mL |
| 5 mM | 0.2740 mL | 1.3698 mL | 2.7396 mL | 6.8490 mL | |
| 10 mM | 0.1370 mL | 0.6849 mL | 1.3698 mL | 3.4245 mL | |
| 15 mM | 0.0913 mL | 0.4566 mL | 0.9132 mL | 2.2830 mL | |
| 20 mM | 0.0685 mL | 0.3425 mL | 0.6849 mL | 1.7123 mL | |
| 25 mM | 0.0548 mL | 0.2740 mL | 0.5479 mL | 1.3698 mL | |
| 30 mM | 0.0457 mL | 0.2283 mL | 0.4566 mL | 1.1415 mL | |
| 40 mM | 0.0342 mL | 0.1712 mL | 0.3425 mL | 0.8561 mL | |
| 50 mM | 0.0274 mL | 0.1370 mL | 0.2740 mL | 0.6849 mL | |
| 60 mM | 0.0228 mL | 0.1142 mL | 0.2283 mL | 0.5708 mL | |
| 80 mM | 0.0171 mL | 0.0856 mL | 0.1712 mL | 0.4281 mL | |
| 100 mM | 0.0137 mL | 0.0685 mL | 0.1370 mL | 0.3425 mL |
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