DR 4485 hydrochloride

Pricing Availability   Qty
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)
Citations (3)
Literature (2)

Biological Activity for DR 4485 hydrochloride

DR 4485 hydrochloride is a 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 for DR 4485 hydrochloride

DR 4485 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for DR 4485 hydrochloride

M. Wt 491.88
Formula C26H28Cl2N2O.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 402942-53-4
PubChem ID 90488996
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for DR 4485 hydrochloride

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

Preparing Stock Solutions for DR 4485 hydrochloride

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

Select a batch to recalculate based on the batch molecular weight:
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 for DR 4485 hydrochloride

References for DR 4485 hydrochloride

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

If you know of a relevant reference for DR 4485 hydrochloride, please let us know.

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3 Citations for DR 4485 hydrochloride

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

Gerd et al (2021) Autophagy activation, lipotoxicity and lysosomal membrane permeabilization synergize to promote pimozide- and loperamide-induced glioma cell death. Autophagy 17 3424-3443 PMID: 33461384

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

Thomas C et al (2019) Neuromodulator Signaling Bidirectionally Controls Vesicle Numbers in Human Synapses. Cell 179 498-513.e22 PMID: 31585084

Do you know of a great paper that uses DR 4485 hydrochloride from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

5-HT Receptors Scientific Review

5-HT Receptors Scientific Review

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.

Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.