TargetMol

GSK256471

Product Code:
 
TAR-T32007
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T32007-5mg5mg£1,171.00
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TAR-T32007-50mg50mg£2,303.00
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Quantity:
TAR-T32007-100mg100mg£3,042.00
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Further Information

Bioactivity:
GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Max) response induced by neurokinin B, indicating insurgable antagonist pharmacology (PA (2)=9.2). GSK256471 may be a promising candidate for the treatment of schizophrenia.
CAS:
1133706-08-7
Formula:
C29H29N3O3S
Molecular Weight:
499.63
Purity:
0.98
SMILES:
CN(Cc1c(nc2ccccc2c1C(=O)N[C@@H](C1CC1)c1ccccc1)-c1ccccc1)S(C)(=O)=O

References

1. Dawson LA, Langmead CJ, Dada A, Watson JM, Wu Z, de la Flor R, Jones GA, Cluderay JE, Southam E, Murkitt GS, Hill MD, Jones DN, Davies CH, Hagan JJ, Smith PW. In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics. Eur J Pharmacol. 2010 Feb 10;627(1-3):106-14. doi: 10.1016/j.ejphar.2009.10.054. Epub 2009 Oct 30. PubMed PMID: 19879867. 2. Smith PW, Wyman PA, Lovell P, Goodacre C, Serafinowska HT, Vong A, Harrington F, Flynn S, Bradley DM, Porter R, Coggon S, Murkitt G, Searle K, Thomas DR, Watson JM, Martin W, Wu Z, Dawson LA. New quinoline NK3 receptor antagonists with CNS activity. Bioorg Med Chem Lett. 2009 Feb 1;19(3):837-40. doi: 10.1016/j.bmcl.2008.12.005. Epub 2008 Dec 7. PubMed PMID: 19117759.