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Submit ReviewDR 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.
DR 4485 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 49.19 | 100 |
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.
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 |
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.
Keywords: DR 4485 hydrochloride, DR 4485 hydrochloride supplier, DR4485, hydrochloride, high, affinity, potent, 5-HT-7, selective, serotonin, orally, bioavailable, antagonists, 5-HT7, Receptors, 5005, Tocris Bioscience
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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