DR 4485 hydrochloride

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Cat.No. 5005 - DR 4485 hydrochloride | C26H28Cl2N2O.HCl | CAS No. 402942-53-4
Description: High affinity and selective 5-HT7 antagonist; orally bioavailable
Chemical Name: 6-Chloro-2a-[4-[4-(4-chlorophenyl)-3,6-dihydro-1(2H)-pyridinyl]butyl]-2a,3,4,5-tetrahydrobenz[cd]indol-2(1H)-one hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

High affinity and selective 5-HT7 antagonist (pKi = 8.14). Exhibits selectivity for 5-HT7 over other 5-HT receptors. Inhibits 5-HT-induced cAMP accumulation in HEK-293 cells expressing the 5-HT7 receptor. Orally bioavailable.

Compound Libraries

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Technical Data

M. Wt 491.88
Formula C26H28Cl2N2O.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 402942-53-4
PubChem ID 90488996
InChI Key QAERYGXKDZHTFR-UHFFFAOYSA-N
Smiles ClC1=C2C(C3(CCCCN4CCC(C5=CC=C(Cl)C=C5)=CC4)CCC2)=C(NC3=O)C=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.19 100

Preparing Stock Solutions

The following data is based on the product molecular weight 491.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.03 mL 10.17 mL 20.33 mL
5 mM 0.41 mL 2.03 mL 4.07 mL
10 mM 0.2 mL 1.02 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

Kikuchi et al (2003) New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. Bioorg.Med.Chem.Lett. 13 61 PMID: 12467617

Medina et al (2009) Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. J.Med.Chem. 52 2384 PMID: 19326916


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1 Citation for DR 4485 hydrochloride

Citations are publications that use Tocris products. Selected citations for DR 4485 hydrochloride include:

Chan et al (2016) A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors. PLoS Pathog 12 e1005651 PMID: 27187180


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Literature in this Area

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Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

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