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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- No. CAS: 2043947-71-1
- Fòrmula: C22H22N8
- Peso molecular:398.46
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
6 μM
Compound: 1; MeIm
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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
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[PMID: 31260298] |
Chemical Information
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No. CAS 2043947-71-1
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Peso molecular 398.46
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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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.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MeIm Related Classifications
HY-161941 Related Classifications
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