AChE-IN-9
AChE-IN-9 is a Tacrine (HY-111338) glycoconjugate tethered with acetylated β-Glucose. AChE-IN-9 is also an AChE inhibitor with an IC50 value of 0.4 μM, with lower hepatotoxicity on healthy cells. Tacrine is used in Alzheimer's research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C30H35N5O9
- 分子量:609.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
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AChE 0.4 μM (IC50) |
体外実験
Tacrine (HY-111338) is mainly metabolized by CYP 1A2, but its glycoconjugates have shown more affinity towards CYP 3A4 rather than CYP 1A2[1].
AChE-IN-9 (compound A-1) (200 μM; 24 h) is non-toxic on HePG2 cell line with 100% cell viability, and shows lower hepatotoxicity than Tacrine (HY-111338) on healthy HepG2 cells[1].
AChE-IN-9 (10 μM; 24 h) inhibits AChE activity with inhibition rate of 96.6%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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分子量 609.63
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分子式 C30H35N5O9
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SMILES
CC(OC[C@H]1O[C@@H]([C@@H]([C@H]([C@@H]1OC(C)=O)OC(C)=O)OC(C)=O)N2C=C(N=N2)CNC3=C4CCCCC4=NC5=CC=CC=C53)=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
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Hepatotoxicity Study
This protocol evaluates hepatotoxicity using complementary in vivo mouse APAP acute liver injury and in vitro hepatocyte-based cytotoxicity readouts. In vivo APAP injury is assessed by serum ALT/AST, liver histology, hepatic glutathione, protein adducts, necrosis, inflammation, and regeneration-related endpoints. In vitro hepatotoxicity is assessed by loss of viability, leakage of ALT/AST/LDH, oxidative-stress markers, mitochondrial function, nuclear morphology, intracellular calcium, and high-content imaging endpoints.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)