UPF-648
Based on 1 publication(s) in Google Scholar
UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.
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- 純度: 99.75%
- CAS 番号: 213400-34-1
- 分子式: C11H8Cl2O3
- 分子量:259.09
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 UPF-648
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生物活性
BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity[1].
UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels[2].
UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 213400-34-1
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性状 Solid
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分子量 259.09
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分子式 C11H8Cl2O3
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Color White to off-white
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SMILES
O=C([C@@H]1[C@@H](C(C2=CC=C(Cl)C(Cl)=C2)=O)C1)O
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
UPF 648, a Selective KMO Inhibitor, Attenuates Psychomotor and Cognitive Impairment in Chronic Kidney Disease. [Abstract]2025 Mar 5;16(5):908-919. PMID: 39961731
溶剤 & 溶解度
Ethanol : ≥ 50 mg/mL (192.98 mM)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (274 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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取扱説明書 (2659 KB)
参考文献
[1]. Amori L, et al. On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo. J Neurochem. 2009 Apr;109(2):316-25. [Content Brief]
[2]. Ceresoli-Borroni G, et al. Perinatal kynurenine 3-hydroxylase inhibition in rodents: pathophysiological implications. J Neurosci Res. 2007 Mar;85(4):845-54. [Content Brief]
[3]. Amaral M, et al. Structural basis of kynurenine 3-monooxygenase inhibition. Nature. 2013 Apr 18;496(7445):382-5. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol | 1 mM | 3.8597 mL | 19.2985 mL | 38.5969 mL | 96.4923 mL |
| 5 mM | 0.7719 mL | 3.8597 mL | 7.7194 mL | 19.2985 mL | |
| 10 mM | 0.3860 mL | 1.9298 mL | 3.8597 mL | 9.6492 mL | |
| 15 mM | 0.2573 mL | 1.2866 mL | 2.5731 mL | 6.4328 mL | |
| 20 mM | 0.1930 mL | 0.9649 mL | 1.9298 mL | 4.8246 mL | |
| 25 mM | 0.1544 mL | 0.7719 mL | 1.5439 mL | 3.8597 mL | |
| 30 mM | 0.1287 mL | 0.6433 mL | 1.2866 mL | 3.2164 mL | |
| 40 mM | 0.0965 mL | 0.4825 mL | 0.9649 mL | 2.4123 mL | |
| 50 mM | 0.0772 mL | 0.3860 mL | 0.7719 mL | 1.9298 mL | |
| 60 mM | 0.0643 mL | 0.3216 mL | 0.6433 mL | 1.6082 mL | |
| 80 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 100 mM | 0.0386 mL | 0.1930 mL | 0.3860 mL | 0.9649 mL |
UPF-648 関連分類
HY-15600 関連分類
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