1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor
  3. 5-HT1AR/5-HT6R ligand-1

5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM.

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5-HT1AR/5-HT6R ligand-1 Chemical Structure

5-HT1AR/5-HT6R ligand-1 Chemical Structure

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Description

5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM[1].

IC50 & Target

5-HT1AR

19 nM (Ki)

5-HT6R

69 nM (Ki)

5-HT7R

198 nM (Ki)

D2 Receptor

1903 nM (Ki)

Molecular Weight

485.04

Formula

C25H29ClN4O2S

SMILES

O=S(C1=C2C=CC=CC2=CC=C1Cl)(NCCCCCCNC3=NC4=C(C=CC=C4)C(C)N3)=O

Shipping

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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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.

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Product Name:
5-HT1AR/5-HT6R ligand-1
Cat. No.:
HY-173044
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