TargetMol

Velusetrag

Product Code:
 
TAR-T35046
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T35046-5mg5mg£304.00
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TAR-T35046-50mg50mg£1,267.00
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Quantity:
TAR-T35046-100mg100mg£1,878.00
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This product comes from: United States.
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  • Further Information
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Further Information

Bioactivity:
Velusetrag(TD-5108)is an effective, selective, and highly potent agonist of the 5-HT4 receptor, and being developed for the treatment of gastroparesis, chronic constipation, and irritable bowel syndrome.
CAS:
866933-46-2
Formula:
C25H36N4O5S
Molecular Weight:
504.65
Purity:
0.98
SMILES:
[H]C12CCC([H])(CC(C1)NC(=O)c1cc3ccccc3n(C(C)C)c1=O)N2C[C@@H](O)CN(C)S(C)(=O)=O

References

Beattie DT, Higgins DL, Ero MP, Amagasu SM, Vickery RG, Kersey K, Hopkins A, Smith JA. An in vitro investigation of the cardiovascular effects of the 5-HT(4) receptor selective agonists, velusetrag and TD-8954. Vascul Pharmacol. 2013 Jan;58(1-2):150-6. doi: 10.1016/j.vph.2012.11.002. Epub 2012 Nov 29. PubMed PMID: 23201772. Long DD, Armstrong SR, Beattie DT, Choi SK, Fatheree PR, Gendron RA, Genov D, Goldblum AA, Humphrey PP, Jiang L, Marquess DG, Shaw JP, Smith JA, Turner SD, Vickery RG. Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6048-52. doi: 10.1016/j.bmcl.2012.08.051. Epub 2012 Aug 21. PubMed PMID: 22959244. Shin A, Camilleri M, Kolar G, Erwin P, West CP, Murad MH. Systematic review with meta-analysis: highly selective 5-HT4 agonists (prucalopride, velusetrag or naronapride) in chronic constipation. Aliment Pharmacol Ther. 2014 Feb;39(3):239-53. doi: 10.1111/apt.12571. Epub 2013 Dec 5. Review. PubMed PMID: 24308797. Goldberg M, Li YP, Johanson JF, Mangel AW, Kitt M, Beattie DT, Kersey K, Daniels O. Clinical trial: the efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation - a 4-week, randomized, double-blind, placebo-controlled, dose-response study. Aliment Pharmacol Ther. 2010 Nov;32(9):1102-12. doi: 10.1111/j.1365-2036.2010.04456.x. Epub 2010 Sep 22. PubMed PMID: 21039672.