A 5-HT4 receptor agonist
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Velusetrag

Item No. 45464

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,2-dihydro-N-[(3-endo)-8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]oct-3-yl]-1-(1-methylethyl)-2-oxo-3-quinolinecarboxamide
CAS Number
866933-46-2
Synonyms
  • TD-5108
Molecular Formula
C25H36N4O5S
Formula Weight
504.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/ml
SMILES
[H][C@@]12CC[C@@](C[C@H](C1)NC(C3=CC4=CC=CC=C4N(C(C)C)C3=O)=O)(N2C[C@H](CN(S(=O)(C)=O)C)O)[H]
InChi Code
InChI=1S/C25H36N4O5S/c1-16(2)29-23-8-6-5-7-17(23)11-22(25(29)32)24(31)26-18-12-19-9-10-20(13-18)28(19)15-21(30)14-27(3)35(4,33)34/h5-8,11,16,18-21,30H,9-10,12-15H2,1-4H3,(H,26,31)/t18-,19+,20-,21-/m0/s1
InChi Key
HXLOHDZQBKCUCR-WOZUAGRISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $295

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    10 mg

    $561

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    25 mg

    $1,033

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    50 mg

    $1,770

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    Product Description

    Velusetrag is an agonist of the serotonin (5-HT) receptor subtype 5-HT4.1 It increases cAMP accumulation in HEK293 cells expressing human 5-HT4(c), 5-HT4(d), and 5-HT4(g) receptors (EC50s = 5.01, 2.51, and 6.31 nM, respectively). Velusetrag is greater than 500-fold selective for the 5-HT4 receptor over ten other 5-HT receptors and greater than 25-fold selective over eighteen other non-5-HT biogenic amine receptors at 10 µM. It induces contractions in guinea pig colonic longitudinal muscle-myenteric plexus (LM-MP) preparations (EC50 = 12.59 nM) and relaxation in carbachol-precontracted rat esophagus preparations (EC50 = 12.59 nM). Velusetrag reduces fecal transit time in guinea pigs and increases contractility of the antrum, duodenum, and jejunum in dogs.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smith, J.A., Beattie, D.T., Marquess, D., et al. The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch. Pharmacol. 378(1), 125-137 (2008).

    2. Beattie, D.T., Armstrong, S.R., Shaw, J.P., et al. The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch. Pharmacol. 378(1), 139-147 (2008).