Ibrexafungerp citrate
Based on 1 publication(s) in Google Scholar
Ibrexafungerp citrate (MK 3118 citrate) is an orally active β-1,3-glucan synthesis inhibitor, with potential antifungal activity. Ibrexafungerp citrate is an investigational agent for the treatment of Candida and Aspergillus infections.
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- Pureté : 99.38%
- CAS No.: 1965291-08-0
- Formule: C50H75N5O11
- Masse moléculaire:922.16
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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
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Publications Citing Use of MedChemExpress (MCE) Ibrexafungerp citrate
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Activité biologique
Description
In Vitro
Ibrexafungerp citrate (MK 3118 citrate) leads to fungicidal activity against various Candida spp., with a minimum inhibitory concentration (MIC50) of 0.5 µg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
Ibrexafungerp citrate (MK 3118 citrate) exhibits oral bioavailability (mouse 51%, rat 45%, dog 35%) following oral administration (mouse 1 mg/kg, rat 5 mg/kg and dog 5 mg/kg)[3].
Ibrexafungerp citrate (MK 3118 citrate) 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) combined with large volumes of distribution (5.3, 4.7, and 4.1 L/kg respectively) following intravenous administration (mouse 1 mg/kg, rat 5 mg/kg and dog 5 mg/kg)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 mice, Male and female Han Wister rats, Male and female beagle dogs[3]
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Dosage:Mice (1 mg/kg), rats (5 mg/kg) and dogs (5 mg/kg)
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Administration:Intravenous (i.v.) or oral gavage
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Result:T1/2s of 5.5, 8.7, and 9.3 h for mice, rats, and dogs, respectively.
Chemical Information
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CAS No. 1965291-08-0
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Appearance Solid
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Masse moléculaire 922.16
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Formule C50H75N5O11
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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.OC(CC(C(O)=O)(O)CC(O)=O)=O
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Synonyms
MK 3118 citrate; SCY-078 citrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (108.44 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 (protect from light). 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 (protect from light). 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)
In Vivo:
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 (2.71 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 (2.71 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (283 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]. 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]
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 (protect from light). 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 | 1.0844 mL | 5.4221 mL | 10.8441 mL | 27.1103 mL |
| 5 mM | 0.2169 mL | 1.0844 mL | 2.1688 mL | 5.4221 mL | |
| 10 mM | 0.1084 mL | 0.5422 mL | 1.0844 mL | 2.7110 mL | |
| 15 mM | 0.0723 mL | 0.3615 mL | 0.7229 mL | 1.8074 mL | |
| 20 mM | 0.0542 mL | 0.2711 mL | 0.5422 mL | 1.3555 mL | |
| 25 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | 1.0844 mL | |
| 30 mM | 0.0361 mL | 0.1807 mL | 0.3615 mL | 0.9037 mL | |
| 40 mM | 0.0271 mL | 0.1356 mL | 0.2711 mL | 0.6778 mL | |
| 50 mM | 0.0217 mL | 0.1084 mL | 0.2169 mL | 0.5422 mL | |
| 60 mM | 0.0181 mL | 0.0904 mL | 0.1807 mL | 0.4518 mL | |
| 80 mM | 0.0136 mL | 0.0678 mL | 0.1356 mL | 0.3389 mL | |
| 100 mM | 0.0108 mL | 0.0542 mL | 0.1084 mL | 0.2711 mL |
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