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) .
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.78%
- CAS No.: 1353734-12-9
- Formule: C32H30F3N5O3
- Masse moléculaire:589.61
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Stockage: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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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
Activité biologique
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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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1353734-12-9
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Appearance Solid
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Masse moléculaire 589.61
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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 |
TBI-166 Related Classifications
HY-148564 Related Classifications
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