MeIm
MeIm (compound 7) is a high-affinity PCSK9 targeting peptide mimetic with cholesterol-lowering activity. MeIm increases cellular uptake of LDL (EC50=6.04 μM) by inhibiting the binding of PCSK9 to LDLR (IC50=11.2 μM). MeIm can be used in the study of cardiovascular diseases.
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- CAS 番号: 2043947-71-1
- 分子式: C22H22N8
- 分子量:398.46
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
6 μM
Compound: 1; MeIm
|
Inhibition of PCSK9 (unknown origin) interaction with LDLR expressed in human HepG2 cells assessed as increase in LDL uptake level measured after 24 hrs by LDL-Dylight 550 dye based fluorescence assay
Inhibition of PCSK9 (unknown origin) interaction with LDLR expressed in human HepG2 cells assessed as increase in LDL uptake level measured after 24 hrs by LDL-Dylight 550 dye based fluorescence assay
|
[PMID: 31260298] |
化学情報
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CAS 番号 2043947-71-1
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分子量 398.46
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分子式 C22H22N8
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SMILES
CN1C(C2=CC=CC=C2)=CN=C1C3=CN=C(C4=CN=C(C5=CN=CN5C)N4C)N3C
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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.
純度とドキュメンテーション
参考文献
[1]. Xuhui Bao, et al. "Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside." Signal Transduction and Targeted Therapy 9.1 (2024): 13. [Content Brief]
[2]. Stucchi, et al. "Disrupting the PCSK9/LDLR protein–protein interaction by an imidazole-based minimalist peptidomimetic." Organic & Biomolecular Chemistry 14.41 (2016): 9736-9740. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)