ReN-1869 hydrochloride
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
For research use only. We do not sell to patients.
- CAS No.: 170149-76-5
- Formula: C24H28ClNO2
- Molecular Weight:397.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
All Histamine Receptor Isoforms
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Biological Activity
Ki: 0.19±0.04 μM (histamine H1 receptor)[1]
ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H1 receptor antagonism. Binding studies with radioactively labelled ReN 1869 reveals high affinity only for the histamine H1 receptor in addition to some affinity for a sigma site. ReN 1869 is profiled for activity at 10 μM at various receptors, transporters, enzymes and ion channels. ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain, [3H]pyrilamine) with a Ki of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [3H]1,3-di-tolylguanidine (DTG)] with a Ki of 0.45 μM. ReN 1869 dose-dependently reduces the responses with IC50 of 1.70±0.002 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 170149-76-5
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Molecular Weight 397.94
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Formula C24H28ClNO2
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SMILES
O=C([C@H]1CN(CC/C=C2C3=CC=CC=C3CCC4=CC=CC=C\24)CCC1)O.[H]Cl
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Synonyms
NNC-05-1869 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
ReN 1869 is labelled with 3H in the tricyclic ring system resulting in a specific activity of 40 Ci/mmol. Thawed membranes (1 mg protein/tube), test compounds and [3H]ReN 1869 are added to test tubes in a final volume of 0.5 mL. Unless otherwise indicated, the concentration of the radioligand is 5 nM and non-specific binding is defined as the binding in the presence of 10 μM ReN 1869. Samples are incubated for 120 min at 37 °C in a shaking water bath. Free and bound radioactivity is separated by filtration over Whatman GF/F filters that are washed with 25 mL of ice-cold buffer (20 mM Tris-HCl, pH 7.4). Radioligand bound to filters accounted for 5-700 dpm that is subtracted before calculating specific binding[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ReN-1869 hydrochloride Related Classifications
HY-101724 Related Classifications
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