DA-6886 monohydrochloride
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome.
For research use only. We do not sell to patients.
- CAS No.: 1645260-76-9
- Formula: C19H28Cl2N6O2
- Molecular Weight:443.37
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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5-HT4 Receptor 4.3 (pIC50) |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1645260-76-9
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Molecular Weight 443.37
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Formula C19H28Cl2N6O2
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SMILES
O=C(NCC1CCN(CCCN2N=NC=C2)CC1)C3=CC(Cl)=C(N)C=C3OC.Cl
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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.
Protocols
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Two-electrode voltage clamp in Xenopus oocytes
Two-electrode voltage clamp measures whole-oocyte membrane current from Xenopus oocytes expressing exogenous ion channels, receptors, or transporters; one intracellular microelectrode senses membrane voltage, and the second injects current so the amplifier can hold the membrane at command voltages while recording the compensating current as the functional readout. The method is suited to Xenopus oocytes because their large size supports microinjection and intracellular electrode impalement, but the large membrane area can limit voltage-clamp speed and accuracy, especially for large or fast currents.
Purity & Documentation
References
[1]. Lee D Y, et al. Pharmacokinetics of DA-6886, a new 5-HT4 receptor agonist, in rats[J]. Pharmaceutics, 2022, 14(4): 702. [Content Brief]
[2]. Lee M J, et al. Pharmacological profile of DA-6886, a novel 5-HT4 receptor agonist to accelerate colonic motor activity in mice[J]. European Journal of Pharmacology, 2014, 735: 115-122. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DA-6886 monohydrochloride Related Classifications
HY-19927A Related Classifications
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