TBI-166
Based on 1 Customer Validation
TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine (HY-B1046) .
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: 99.78%
- CAS 番号: 1353734-12-9
- 分子式: C32H30F3N5O3
- 分子量:589.61
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | IC50 |
>64 μg/mL
Compound: 78
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Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
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[PMID: 22931472] |
TBI-166 inhibits M. tuberculosis H37Rv replicates (MIC: 0.063 μg/mL), and is effective against 16 drug-sensitive clinical isolates (Mycobacterial species) with MICs of 0.005-0.15 μg/mL[1].
TBI-166 (0-1 μg/mL, 3 days) inhibits intracellular M. tuberculosis in M. tuberculosis infecting J774A.1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TBI-166 displays a LD50 more than 3,000 mg/kg in mice[1].
TBI-166 has a short half-life (41.25 h) and reduces the potential for skin pigmentation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic murine M. tuberculosis H37Rv infected model[1]
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Dosage:10, 20, 80 mg/kg
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Administration:Oral administration, 8 weeks.
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Result:Reduced CFU counts in lung.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1353734-12-9
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性状 Solid
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分子量 589.61
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分子式 C32H30F3N5O3
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Color Brown to reddish brown
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SMILES
FC(F)(F)OC1=CC=C(N2C3=C/C(C(NC4=CC=CN=C4OC)=CC3=NC5=C2C=CC=C5)=N/C6CCC(OC)CC6)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 9.09 mg/mL (15.42 mM; ultrasonic and adjust pH to 3 with 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.
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
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データシート (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Xu J, et al. In Vitro and In Vivo Activities of the Riminophenazine TBI-166 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2019 Apr 25;63(5):e02155-18. [Content Brief]
[2]. Zhu H, et al. Activity of Clofazimine and TBI-166 against Mycobacterium tuberculosis in Different Administration Intervals in Mouse Tuberculosis Models. Antimicrob Agents Chemother. 2021 Mar 18;65(4):e02164-20. [Content Brief]
[3]. Ding Y, et al. Superior Efficacy of a TBI-166, Bedaquiline, and Pyrazinamide Combination Regimen in a Murine Model of Tuberculosis. Antimicrob Agents Chemother. 2022 Sep 20;66(9):e0065822. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6960 mL | 8.4802 mL | 16.9604 mL | 42.4009 mL |
| 5 mM | 0.3392 mL | 1.6960 mL | 3.3921 mL | 8.4802 mL | |
| 10 mM | 0.1696 mL | 0.8480 mL | 1.6960 mL | 4.2401 mL | |
| 15 mM | 0.1131 mL | 0.5653 mL | 1.1307 mL | 2.8267 mL |