TargetMol

PF-4455242

Product Code:
 
TAR-T28383
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T28383-5mg5mg£850.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
TAR-T28383-50mg50mg£1,661.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
TAR-T28383-100mg100mg£2,079.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
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  • Further Information
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Further Information

Bioactivity:
PF-4455242 is a selective, short-acting antagonist of the κ-opioid receptor.
CAS:
1322001-35-3
Formula:
C21H29ClN2O2S
Molecular Weight:
408.99
Purity:
0.98
SMILES:
Cl.CC(C)CNCc1ccc(cc1)-c1ccccc1S(=O)(=O)N1CCCC1

References

1. Naganawa M, Jacobsen LK, Zheng MQ, Lin SF, Banerjee A, Byon W, Weinzimmer D, Tomasi G, Nabulsi N, Grimwood S, Badura LL, Carson RE, McCarthy TJ, Huang Y. Evaluation of the agonist PET radioligand [??C]GR103545 to image kappa opioid receptor in humans: kinetic model selection, test-retest reproducibility and receptor occupancy by the antagonist PF-04455242. Neuroimage. 2014 Oct 1;99:69-79. doi: 10.1016/j.neuroimage.2014.05.033. Epub 2014 May 17. PubMed PMID: 24844744; PubMed Central PMCID: PMC4140089. 2. Sawant Basak A, Byon W, Tseng-Lovering E, Funk C, Wood L, Lin C, Delnomdedieu M, Verhoest P, Parikh V, Cox LM, Miller E, Gao H, Obach RS. Metabolism and clinical pharmacokinetics of 2-methyl-n-(2'-(pyrrolidinyl-1-ylsulfonyl)-n-[1,1'-biphenyl]-4-yl)propran-1-amine : insights into monoamine oxidase- and CYP-mediated disposition by integration of in vitro ADME tools. Xenobiotica. 2014 May;44(5):438-54. doi: 10.3109/00498254.2013.850552. Epub 2013 Dec 4. PubMed PMID: 24304147. 3. Hu S, Yu H, Liu Y, Xue T, Zhang H. Insight into the binding model of new antagonists of kappa receptor using docking and molecular dynamics simulation. J Mol Model. 2013 Aug;19(8):3087-94. doi: 10.1007/s00894-013-1839-3. Epub 2013 Apr 20. PubMed PMID: 23605139. 4. Chang C, Byon W, Lu Y, Jacobsen LK, Badura LL, Sawant-Basak A, Miller E, Liu J, Grimwood S, Wang EQ, Maurer TS. Quantitative PK-PD model-based translational pharmacology of a novel kappa opioid receptor antagonist between rats and humans. AAPS J. 2011 Dec;13(4):565-75. doi: 10.1208/s12248-011-9296-3. Epub 2011 Aug 17. PubMed PMID: 21847689; PubMed Central PMCID: PMC3231851.