MK-7762
Based on 1 Customer Validation
MK-7762 is an orally active xazolidinone compound with antitubercular activity. MK-7762 inhibits MAO-B and mammalian mitochondrial protein synthesis. MK-7762 reduces lung bacterial burden in BALB/c mouse models of acute and chronic tuberculosis infection, penetrates caseous necrotic lung lesions in C3HeB/FeJ mice, and maintains concentrations above unbound MIC in lesion compartments. MK-7762 can be used for the research of tuberculosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.97%
- CAS 番号: 2706576-88-5
- 分子式: C16H19F2N3O6S
- 分子量:419.40
-
保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
体外実験
MK-7762 (0.93 μM; 7 days) inhibits 95% of Mycobacterium tuberculosis (Mtb) growth[1].
MK-7762 (72 h) inhibits mammalian mitochondrial protein synthesis in HepG2 cells with an IC50 of 98 μM[1].
MK-7762 (18.1 μM; 7 days) kills 99% of H37Rv cells [1].
MK-7762 (10 μM) inhibits MAO-B with an IC50 of 6.9 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MK-7762 (30-200 mg/kg; i.g.; once daily; 1 month) reduces lung bacterial burden in chronically infected BALB/c mice[1].
MK-7762 (100 mg/kg; i.g.; once daily, 5 days/week; 2.5 weeks) penetrates caseous necrotic lesions in C3HeB/FeJ mice at levels above the unbound MIC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c (female, 6-8 weeks old, specific-pathogen-free, acute Mtb infection)[1]
-
Dosage:30 mg/kg; 100 mg/kg
-
Administration:I.g.; once daily, twice daily; 12 days
-
Result:Achieved 1.4-log reduction in lung CFUs (30 mg/kg once daily).
Achieved 4.5-log reduction in lung CFUs (100 mg/kg once daily).
Achieved 5.3-log reduction in lung CFUs (100 mg/kg twice daily) versus untreated controls.
-
Animal Model:BALB/c (female, 6-8 weeks old, specific-pathogen-free, chronic Mtb infection)[1]
-
Dosage:30 mg/kg; 100 mg/kg; 200 mg/kg
-
Administration:I.g.; once daily; 1 month
-
Result:Achieved 0.7-log reduction in lung CFUs (30 mg/kg).
Achieved 1.9-log reduction in lung CFUs (100 mg/kg).
Achieved 2.2-log reduction in lung CFUs (200 mg/kg) versus untreated controls.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 2706576-88-5
-
性状 Solid
-
分子量 419.40
-
分子式 C16H19F2N3O6S
-
Color White to off-white
-
SMILES
COC(NC[C@H]1CN(C(O1)=O)C2=CC(F)=C(C(F)=C2)N3CCS(=O)(CC3)=O)=O
-
別名
TBD09
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (238.44 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
参考文献
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 | 2.3844 mL | 11.9218 mL | 23.8436 mL | 59.6090 mL |
| 5 mM | 0.4769 mL | 2.3844 mL | 4.7687 mL | 11.9218 mL | |
| 10 mM | 0.2384 mL | 1.1922 mL | 2.3844 mL | 5.9609 mL | |
| 15 mM | 0.1590 mL | 0.7948 mL | 1.5896 mL | 3.9739 mL | |
| 20 mM | 0.1192 mL | 0.5961 mL | 1.1922 mL | 2.9804 mL | |
| 25 mM | 0.0954 mL | 0.4769 mL | 0.9537 mL | 2.3844 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7948 mL | 1.9870 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5961 mL | 1.4902 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4769 mL | 1.1922 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9935 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7451 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5961 mL |
MK-7762 関連分類
HY-181146 関連分類
Powered by Bioz