JNJ-6640
Based on 1 Customer Validation
JNJ-6640 is an inhibitor targeting mycobacterial PurF (the first enzyme in the de novo purine biosynthesis pathway) with potent anti-tuberculosis activity. JNJ-6640 exhibits bactericidal activity against Mycobacterium tuberculosis in vitro, with an MIC90 of 8.6 nM. JNJ-6640 disrupts de novo purine biosynthesis, inhibits M. tuberculosis DNA replication in vivo. JNJ-6640 exhibits anti-tuberculosis efficacy in acutely infected mice. JNJ-6640 can be used for the study of tuberculosis.
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- Purity: 99.72%
- 화학식: C17H17FN6O
- 분자량:340.35
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
JNJ-6640 exhibits potent in vitro inhibitory and bactericidal activity against Mycobacterium tuberculosis H37Rv strain, with a minimum inhibitory concentration (MIC90) of 8.6 nM and a minimum bactericidal concentration (MBC99.9) of 140 nM; in cholesterol medium, (MIC90) is 29.1 nM; for intracellular M. tuberculosis in THP-1 macrophages IC50 is 26.1 nM[1].
JNJ-6640 (100 nM, 4 h) significantly reduces the incorporation ratio of 15N into adenine and adenosine monophosphate (AMP) in M. tuberculosis[1].
JNJ-6640 (1 nM) inhibits M. tuberculosis PurF enzyme[1].
JNJ-6640 (0.6 μM, 6-10 h) arrests the growth of M. tuberculosis expressing TdTomato[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | AUClast | AUCinf | Vss | Vz | MRT | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 64.7 mL/min/kg | 0.16 h | 257 ng·h/mL | 258 ng·h/mL | 0.75 L/kg | 0.90 L/kg | 0.19 h | / | / | / |
| Mice[1] | 1500 mg/kg | s.c. | / | 286 h | 613000 ng·h/mL | 723000 ng·h/mL | / | / | / | 12800 ng/mL | 4 h | ＞100 % |
| Mice[1] | 3000 mg/kg | s.c. | / | 134 h | 1500000 ng·h/mL | 1590000 ng·h/mL | / | / | / | 41800 ng/mL | 292 h | ＞100 % |
| Mice[1] | 5 mg/kg | p.o. | / | 0.76 h | 957 ng·h/mL | 959 ng·h/mL | / | / | / | 1063 ng/mL | 0.5 h | 74 % |
| Mice[1] | 50 mg/kg | p.o. | / | 0.58 h | 47575 ng·h/mL | 47608 ng·h/mL | / | / | / | 2600 mL/min/kg | 0.5 h | ＞100 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mycobacterium tuberculosis H37Rv (200 CFU) was intranasally inoculated into 6-8-week-old female Balb/cBy mice to construct an acute tuberculosis infection model[1]
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Dosage:1500 mg/kg
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Administration:s.c. injection of LAI, once weekly for 2, 8 weeks
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Result:Reduced lung bacterial load.
Showed no significant changes in body weight and no obvious clinical signs of toxicity.
Reduced the phosphorylation of molecules related to M. tuberculosis DNA replication in mice.
Chemical Information
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Appearance Solid
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분자량 340.35
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화학식 C17H17FN6O
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Color White to off-white
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SMILES
CC1=NNC(OC2=C(F)C=NC(N3C[C@H](CC3)C4=CC=NC=C4)=N2)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (293.82 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.9382 mL | 14.6908 mL | 29.3815 mL | 73.4538 mL |
| 5 mM | 0.5876 mL | 2.9382 mL | 5.8763 mL | 14.6908 mL | |
| 10 mM | 0.2938 mL | 1.4691 mL | 2.9382 mL | 7.3454 mL | |
| 15 mM | 0.1959 mL | 0.9794 mL | 1.9588 mL | 4.8969 mL | |
| 20 mM | 0.1469 mL | 0.7345 mL | 1.4691 mL | 3.6727 mL | |
| 25 mM | 0.1175 mL | 0.5876 mL | 1.1753 mL | 2.9382 mL | |
| 30 mM | 0.0979 mL | 0.4897 mL | 0.9794 mL | 2.4485 mL | |
| 40 mM | 0.0735 mL | 0.3673 mL | 0.7345 mL | 1.8363 mL | |
| 50 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4691 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4897 mL | 1.2242 mL | |
| 80 mM | 0.0367 mL | 0.1836 mL | 0.3673 mL | 0.9182 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7345 mL |
JNJ-6640 Related Classifications
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