| 产品描述: | 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. |
| 体外研究: |
Pharmacokinetic Analysis 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]. |
| 体内研究: |
Ibrexafungerp citrate (MK 3118 citrate) leads to fungicidal activity against various Candida spp., with a minimum inhibitory concentration (MIC50) of 0.5 µg/mL. |
| 参考文献: |
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. 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. 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. |
| 保存条件: |
4°C, 避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.084 ml |
5.422 ml |
10.844 ml |
| 5 mM |
0.217 ml |
1.084 ml |
2.169 ml |
| 10 mM |
0.108 ml |
0.542 ml |
1.084 ml |
| 50 mM |
0.022 ml |
0.108 ml |
0.217 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |