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DA-6886 is an agonist 5-Hydroxytryptamine receptor 4 (5-HT4). DA-6886 induced 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 revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $140 | In Stock | |
5 mg | $340 | In Stock | |
10 mg | $510 | In Stock | |
25 mg | $828 | In Stock | |
50 mg | $1,150 | In Stock | |
100 mg | $1,550 | In Stock | |
500 mg | $2,970 | In Stock |
Description | DA-6886 is an agonist 5-Hydroxytryptamine receptor 4 (5-HT4). DA-6886 induced 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 revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels. |
In vivo | In the normal ICR mice, DA-6886 (0.4 and 2mg/kg; oral) resulted in a marked stimulation of colonic transit. In the loperamide-induced constipation mouse model, DA-6886 (2mg/kg) significantly improved the delay of colonic transit. Taken together, DA-6886 is a highly potent and selective 5-HT4 receptor agonist to accelerate colonic transit in mice, which might be a therapeutic agent having a favorable safety profile in the treatment of gastrointestinal motor disorders such as IBS-C and chronic constipation.[1] |
Alias | DA6886, DA 6886 |
Molecular Weight | 443.37 |
Formula | C19H28Cl2N6O2 |
Cas No. | 1645260-76-9 |
Smiles | Cl.O=C(NCC1CCN(CCCN2N=NC=C2)CC1)C3=CC(Cl)=C(N)C=C3OC |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (101.5 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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