Telacebec
Based on 7 publication(s) in Google Scholar
Telacebec (Q203) is a midazopyridine amide compound. Telacebec is active against Mycobacterium tuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium.
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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: 99.40%
- CAS 番号: 1334719-95-7
- 分子式: C29H28ClF3N4O2
- 分子量:557.01
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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
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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MedChemExpress（MCE）の使用を引用している文献 Telacebec
More- Eur J Med Chem. 2022 Nov 15:242:114639. [Abstract]
- Int J Mol Sci. 2022 Sep 7;23(18):10331. [Abstract]
- ACS Infect Dis. 2021 Jan 8;7(1):141-152. [Abstract]
- Antimicrob Agents Chemother. 2021 Aug 17;65(9):e0095621. [Abstract]
- Microbiol Spectr. 2023 Dec 12;11(6):e0228223. [Abstract]
- bioRxiv. 2024 June 11.
- Elife. 2021 Nov 25;10:e69418. [Abstract]
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生物活性
MIC50: 2.7 nM (Mycobacterium tuberculosis H37Rv)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | CC50 |
>100 μM
Compound: Q203
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Cytotoxicity against African green monkey Vero cells measured after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells measured after 72 hrs by MTT assay
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[PMID: 30654236] |
| Vero | CC50 |
>64 μg/mL
Compound: Q203
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 30692025] |
| Vero | IC50 |
>100 μM
Compound: 3, Q203
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Cytotoxicity against African green monkey Vero cells after 72 hrs by CCK8 assay
Cytotoxicity against African green monkey Vero cells after 72 hrs by CCK8 assay
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[PMID: 26191372] |
| Vero | IC50 |
>100 μM
Compound: 44; Q203
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Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay
Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay
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[PMID: 34046598] |
Imidazopyridine amide (IPA) compounds block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. The optimized IPA compound Telacebec (Q203) inhibits the growth of MDR and XDR Mycobacterium tuberculosis clinical isolates in culture broth medium in the low nanomolar range. Telacebec is active against the reference strain Mycobacterium tuberculosis H37Rv with MIC50s of 2.7 nM in culture broth medium and 0.28 nM inside macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1334719-95-7
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性状 Solid
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分子量 557.01
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分子式 C29H28ClF3N4O2
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Color White to off-white
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SMILES
O=C(C1=C(CC)N=C2C=CC(Cl)=CN21)NCC3=CC=C(N4CCC(C5=CC=C(OC(F)(F)F)C=C5)CC4)C=C3
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別名
Q203; IAP6
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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
Publications (7)
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Journal Impact Factor
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Most Recent
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Eur J Med Chem
Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase. [Abstract]2022 Nov 15:242:114639. PMID: 35973312 -
Int J Mol Sci
2022 Sep 7;23(18):10331. PMID: 36142240
Telacebec purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Sep 7;23(18):10331. [Abstract]
M. smegmatis wild-type (WT) and M. smegmatis mutant strain with knocked-out cytochrome bd (bd-KO) in the presence and absence of indicated Q203 (Telacebec, 0-10 μM, 0-80 h) concentrations.
Telacebec purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Sep 7;23(18):10331. [Abstract]
The outgrowth of M. smegmatis bd-KO in presence of Q203 is not due to selection of mutant harboring compensatory mutations. After eventual growth resumption in presence of Q203 (Telacebec) at ~40 h (green curve), the bacteria were re-treated with Q203 (Telacebec) by diluting into fresh 7H9 complete medium containing the drug (blue curve) or re-grown in drug-free 7H9 complete medium for 16 h, and subsequently again diluted into fresh 7H9 complete medium containing the drug.
Telacebec purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Sep 7;23(18):10331. [Abstract]
Quantification of surviving M. smegmatis bd-KO after exposure to Q203 (Telacebec, 10 μM, 0-48 h) in 7H9 complete medium for the indicated time. Colony forming units (CFU/mL) were subsequently counted on agar plates after three days of incubation at 37 °C. Data are Mean ± SD from two independent experiments (biological replicates), each comprising three technical replicates.
Telacebec purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Sep 7;23(18):10331. [Abstract]
Representative dilution series of M. smegmatis bd-KO after exposure to Q203 (Telacebec) in 7H9 complete medium for the indicated time. Each spot represents a 5 µL aliquot.
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ACS Infect Dis
Two-Way Regulation of MmpL3 Expression Identifies and Validates Inhibitors of MmpL3 Function in Mycobacterium tuberculosis. [Abstract]2021 Jan 8;7(1):141-152. PMID: 33319550 -
Antimicrob Agents Chemother
Nitric Oxide-Dependent Electron Transport Chain Inhibition by the Cytochrome bc1 Inhibitor and Pretomanid Combination Kills Mycobacterium tuberculosis. [Abstract]2021 Aug 17;65(9):e0095621. PMID: 34152815 -
Microbiol Spectr
GaMF1.39's antibiotic efficacy and its enhanced antitubercular activity in combination with clofazimine, Telacebec, ND-011992, or TBAJ-876. [Abstract]2023 Dec 12;11(6):e0228223. PMID: 37982630 -
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Elife
Structure of Mycobacterium tuberculosis cytochrome bcc in complex with Q203 and TB47, two anti-TB drug candidates. [Abstract]2021 Nov 25;10:e69418. PMID: 34819223
Telacebec purchased from MedChemExpress. Usage Cited in: Elife. 2021 Nov 25;10:e69418. [Abstract]
Rate of O2 reduction by the hybrid supercomplex before and after addition of Q203(Telacebec).
溶剤 & 溶解度
DMSO : 20 mg/mL (35.91 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. 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (3.59 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
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.
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.
プロトコル
Rats: Sprague Dawley rats are used for pharmacokinetic studies. Compounds (Q203) are given at a dose of 2 mg per kg body weight intravenously or 10 mg per kg body weight orally. The compounds (Q203) are formulated in 20% TPGS (d-α tocopheryl polyethylene glycol 1000 succinate) for repeated-dose studies and in 40% PEG400, pH4 for single-dose studies. Blood samples are taken through the caudal vena cava using 1-mL syringes before perfusion. Samples are collected from three mice or rats at 0.5, 1, 2, 6, 12, 24 and 48 h post-dose. Blood samples are centrifuged at 3,200g for 10 min at 4 °C. Following centrifugation, plasma is collected and frozen until further analysis. Compound concentrations are determined by LC-MS[1].
Mice: Efficacy of Q203 in a mouse model of established tuberculosis is studied. Bacterial loads are enumerated in the lung of infected mice after 14 d and 28 d of treatment. Q203 is used at 0.4, 2 and 10 mg per kg body weight. Bedaquiline and isoniazid (INH) are used as positive controls at 6.5 and 15 mg per kg body weight, respectively. Five mice per group and per time point are used[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (273 KB)
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取扱説明書 (2659 KB)
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. 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 | 1.7953 mL | 8.9765 mL | 17.9530 mL | 44.8825 mL |
| 5 mM | 0.3591 mL | 1.7953 mL | 3.5906 mL | 8.9765 mL | |
| 10 mM | 0.1795 mL | 0.8976 mL | 1.7953 mL | 4.4882 mL | |
| 15 mM | 0.1197 mL | 0.5984 mL | 1.1969 mL | 2.9922 mL | |
| 20 mM | 0.0898 mL | 0.4488 mL | 0.8976 mL | 2.2441 mL | |
| 25 mM | 0.0718 mL | 0.3591 mL | 0.7181 mL | 1.7953 mL | |
| 30 mM | 0.0598 mL | 0.2992 mL | 0.5984 mL | 1.4961 mL |
Telacebec 関連分類
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