NITD-916
Based on 1 Customer Validation
NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 inhibition of InhA reduces the synthesis of mycolic acids and results in cell death. NITD-916 has potent anti-tuberculosis effects.
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- Purity: 99.83%
- CAS No.: 1614262-83-7
- 화학식: C20H25NO2
- 분자량:311.42
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보관:Powder -20°C, 3 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
IC50: 570 nM (InhA)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
>20 μM
Compound: 30j
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 26544629] |
NITD-916 inhibits Mycobacterium tuberculosis (Mtb) with a MIC50 of 50 nM. The MIC activity of NITD-916 against the MDR-Mtb strains ranged from 0.04 to 0.16 μM[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.
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Animal Model:BALB/c mice were infected intranasally with 103 Mtb H37Rv[1].
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Dosage:100 mg/kg
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Administration:p.o.; daily ; 1 month
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Result:Reduced the bacterial burden by 0.95 log in the lung.
Chemical Information
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CAS No. 1614262-83-7
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Appearance Solid
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분자량 311.42
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화학식 C20H25NO2
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Color White to off-white
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SMILES
O=C1C(C2=CC=CC=C2)=C(O)C=C(CC3CCC(C)(C)CC3)N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 17.5 mg/mL (56.19 mM; ultrasonic and warming and heat to 60°C; 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)
순도&문서
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Data Sheet (272 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
[1]. Ujjini H Manjunatha, et al. Direct inhibitors of InhA are active against Mycobacterium tuberculosis. Sci Transl Med. 2015 Jan 7;7(269):269ra3. [Content Brief]
[2]. Matthew B McNeil, et al. Mechanisms of resistance against NITD-916, a direct inhibitor of Mycobacterium tuberculosis InhA. Tuberculosis (Edinb). 2017 Dec;107:133-136. [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 | 3.2111 mL | 16.0555 mL | 32.1110 mL | 80.2774 mL |
| 5 mM | 0.6422 mL | 3.2111 mL | 6.4222 mL | 16.0555 mL | |
| 10 mM | 0.3211 mL | 1.6055 mL | 3.2111 mL | 8.0277 mL | |
| 15 mM | 0.2141 mL | 1.0704 mL | 2.1407 mL | 5.3518 mL | |
| 20 mM | 0.1606 mL | 0.8028 mL | 1.6055 mL | 4.0139 mL | |
| 25 mM | 0.1284 mL | 0.6422 mL | 1.2844 mL | 3.2111 mL | |
| 30 mM | 0.1070 mL | 0.5352 mL | 1.0704 mL | 2.6759 mL | |
| 40 mM | 0.0803 mL | 0.4014 mL | 0.8028 mL | 2.0069 mL | |
| 50 mM | 0.0642 mL | 0.3211 mL | 0.6422 mL | 1.6055 mL |
NITD-916 Related Classifications
HY-122643 Related Classifications
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