ACHN-975 TFA
Based on 1 publication(s) in Google Scholar
ACHN-975 TFA is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL).
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- 純度: 99.02%
- CAS 番号: 1410809-37-8
- 分子式: C22H24F3N3O6
- 分子量:483.44
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 ACHN-975 TFA
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生物活性
IC50: LpxC[1]
ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM[1].ACHN-975 is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively[1].ACHN-975 is potently against the?P. aeruginosa?isolates tested, inhibiting 100% of the isolates at an MIC of ≤2?μg/ml. It against?Pseudomonas aeruginosa?with an MIC50?and MIC90?of 0.06 and 0.25?μg/ml, respectively[2].ACHN-975?is?against six?P. aeruginosa?isolates, it against P. aeruginosa?APAE1064, APAE1232, and APAE1064?isolates with MIC values of 0.12, 0.06?and 0.06??μg/ml, respectively[2].LpxC is highly conserved in gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis. LpxC is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase[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:Neutropenic mouse thigh model with P. aeruginosa ATCC 27853[2]
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Dosage:5-30 mg/kg
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Administration:Intraperitoneal administration; single dose
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Result:Had a bactericidal activity and was against the P. aeruginosa ATCC27853 strain in vivo.
化学情報
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CAS 番号 1410809-37-8
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性状 Solid
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分子量 483.44
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分子式 C22H24F3N3O6
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Color Light yellow to yellow
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SMILES
O=C(N[C@H](C(NO)=O)C(C)(N)C)C1=CC=C(C#CC#C[C@H]2[C@H](CO)C2)C=C1.O=C(O)C(F)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Infect Dis
Genetic and Chemical Screening Reveals Targets and Compounds to Potentiate Gram-Positive Antibiotics against Gram-Negative Bacteria. [Abstract]2022 Oct 14;8(10):2187-2197. PMID: 36098580
溶剤 & 溶解度
DMSO : 100 mg/mL (206.85 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kalinin DV, et al. Insights into the Zinc-Dependent Deacetylase LpxC: Biochemical Properties and Inhibitor Design. Curr Top Med Chem. 2016;16(21):2379-430. [Content Brief]
[2]. Krause KM,et al. Potent LpxC Inhibitors with In Vitro Activity against Multidrug-Resistant Pseudomonas aeruginosa.Antimicrob Agents Chemother. 2019 Oct 22;63(11). pii: e00977-19. [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 (sealed storage, away from moisture). 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 | 2.0685 mL | 10.3425 mL | 20.6851 mL | 51.7127 mL |
| 5 mM | 0.4137 mL | 2.0685 mL | 4.1370 mL | 10.3425 mL | |
| 10 mM | 0.2069 mL | 1.0343 mL | 2.0685 mL | 5.1713 mL | |
| 15 mM | 0.1379 mL | 0.6895 mL | 1.3790 mL | 3.4475 mL | |
| 20 mM | 0.1034 mL | 0.5171 mL | 1.0343 mL | 2.5856 mL | |
| 25 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0685 mL | |
| 30 mM | 0.0690 mL | 0.3448 mL | 0.6895 mL | 1.7238 mL | |
| 40 mM | 0.0517 mL | 0.2586 mL | 0.5171 mL | 1.2928 mL | |
| 50 mM | 0.0414 mL | 0.2069 mL | 0.4137 mL | 1.0343 mL | |
| 60 mM | 0.0345 mL | 0.1724 mL | 0.3448 mL | 0.8619 mL | |
| 80 mM | 0.0259 mL | 0.1293 mL | 0.2586 mL | 0.6464 mL | |
| 100 mM | 0.0207 mL | 0.1034 mL | 0.2069 mL | 0.5171 mL |