2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT6/5-HT2A receptor ligand-2

5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.

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5-HT6/5-HT2A receptor ligand-2 Chemical Structure

5-HT6/5-HT2A receptor ligand-2 Chemical Structure

CAS No. : 2411088-16-7

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5-HT6/5-HT2A receptor ligand-2 Related Antibodies

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Description

5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties[1].

IC50 & Target[1]

5-HT6 Receptor

25 nM (Ki)

5-HT2A Receptor

32 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
5.14 μM
Compound: 42; PKSN-279
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by presto-blue assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by presto-blue assay
[PMID: 31734022]
HepG2 IC50
6.2 μM
Compound: 42; PKSN-279
Cytotoxicity against human HepG2 cells after 24 hrs by ToxiLight bioassay
Cytotoxicity against human HepG2 cells after 24 hrs by ToxiLight bioassay
[PMID: 31734022]
Molecular Weight

351.37

Formula

C20H18FN3O2
CAS No.
SMILES

OC1=CC=C(C2=CC=C(CNCCC3=CNC4=NC=C(F)C=C43)O2)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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5-HT6/5-HT2A receptor ligand-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

5-HT6/5-HT2A receptor ligand-22411088-16-75-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorcognitive dysfunctionInhibitorinhibitorinhibit

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