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DA-6886

DA-6886
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.
Catalog No. T27117Cas No. 1645260-76-9
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Purity:99.89%
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DA-6886

Catalog No. T27117Cas No. 1645260-76-9
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.
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Pack SizePriceAvailabilityQuantity
1 mg$140In Stock
5 mg$340In Stock
10 mg$510In Stock
25 mg$828In Stock
50 mg$1,150In Stock
100 mg$1,550In Stock
500 mg$2,970In Stock
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Product Introduction

Bioactivity
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]
AliasDA6886, DA 6886
Chemical Properties
Molecular Weight443.37
FormulaC19H28Cl2N6O2
Cas No.1645260-76-9
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2555 mL11.2773 mL22.5545 mL112.7726 mL
5 mM0.4511 mL2.2555 mL4.5109 mL22.5545 mL
10 mM0.2255 mL1.1277 mL2.2555 mL11.2773 mL
20 mM0.1128 mL0.5639 mL1.1277 mL5.6386 mL
50 mM0.0451 mL0.2255 mL0.4511 mL2.2555 mL
100 mM0.0226 mL0.1128 mL0.2255 mL1.1277 mL

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