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Felcisetrag

Felcisetrag
Felcisetrag (TD-8954) is a potent and selective orally active 5-HT4 agonist with gastrointestinal prokinetic properties.Felcisetrag shows high affinity for the human recombinant 5-HT4(c) (h5-HT4(c)) receptor with a pKi of 9.4.
Catalog No. T28934Cas No. 916075-84-8
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Felcisetrag

Catalog No. T28934Alias TD-8954, TD8954, TD 8954Cas No. 916075-84-8

Felcisetrag (TD-8954) is a potent and selective orally active 5-HT4 agonist with gastrointestinal prokinetic properties.Felcisetrag shows high affinity for the human recombinant 5-HT4(c) (h5-HT4(c)) receptor with a pKi of 9.4.
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Pack SizePriceAvailabilityQuantity
1 mg$157In Stock
5 mg$397In Stock
10 mg$589In Stock
25 mg$945In Stock
50 mg$1,280In Stock
100 mg$1,730In Stock
500 mg$3,460In Stock
1 mL x 10 mM (in DMSO)$437In Stock
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Product Introduction

Bioactivity
Description
Felcisetrag (TD-8954) is a potent and selective orally active 5-HT4 agonist with gastrointestinal prokinetic properties.Felcisetrag shows high affinity for the human recombinant 5-HT4(c) (h5-HT4(c)) receptor with a pKi of 9.4.
Targets&IC50
5-HT4C receptor (human):9.4 (pKi)
In vitro
Felcisetrag induces an increase in cAMP levels in HEK-293 cells expressing the h5-HT4(c) receptor (pEC50 = 9.3) and elicits contractions in the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50 = 8.6). In vitro, assays demonstrate that Felcisetrag exhibits moderate intrinsic activity.[1]
In vivo
The administration of Felcisetrag (0.033 mg/kg; s.c.) results in an acceleration of carmine red dye colonic transit, leading to a decrease in excretion time.[1]
A dose-dependent relaxation of the esophagus is induced by Felcisetrag (0.03~10 mg/kg; intraduodenal administration).[1]
Felcisetrag (10 and 30 μg/kg; p.o) elicits an increase in contractility in the antrum, duodenum, and jejunum.[1]
AliasTD-8954, TD8954, TD 8954
Chemical Properties
Molecular Weight455.59
FormulaC25H37N5O3
Cas No.916075-84-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45.0 mg/mL (98.8 mM ), Sonication and heating to 60℃ are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1950 mL10.9748 mL21.9496 mL109.7478 mL
5 mM0.4390 mL2.1950 mL4.3899 mL21.9496 mL
10 mM0.2195 mL1.0975 mL2.1950 mL10.9748 mL
20 mM0.1097 mL0.5487 mL1.0975 mL5.4874 mL
50 mM0.0439 mL0.2195 mL0.4390 mL2.1950 mL

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