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PF-04455242
CAS No. 1202647-54-8
PF-04455242( PF-4455242 )
Catalog No. M10734 CAS No. 1202647-54-8
PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
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Biological Information
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Product NamePF-04455242
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NoteResearch use only, not for human use.
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Brief DescriptionPF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.
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DescriptionPF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively; shows 20-fold reduced affinity for hMOR and negligible affinity for DOR (Ki>4 uM); demonstrates antidepressant-like efficacy, attenuates the behavioral effects of stress, dose-dependently reduceds the elevation of spiradoline-induced plasma prolactin in rats.Depression Phase 1 Discontinued.
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In Vitro——
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In Vivo——
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SynonymsPF-4455242
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PathwayEndocrinology/Hormones
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TargetOpioid Receptor
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RecptorOpioid Receptor
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Research AreaNeurological Disease
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IndicationDepression
Chemical Information
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CAS Number1202647-54-8
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Formula Weight372.527
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Molecular FormulaC21H28N2O2S
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Purity>98% (HPLC)
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Solubility——
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SMILESCC(C)CNCC1=CC=C(C=C1)C2=CC=CC=C2S(=O)(=O)N3CCCC3
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Chemical Name2-Methyl-N-[[4-(2-pyrrolidin-1-ylsulfonylphenyl)phenyl]methyl]propan-1-amine
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Verhoest PR, et al. J Med Chem. 2011 Aug 25;54(16):5868-77.
2. Grimwood S, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):555-66.
3. Melief EJ, et al. Mol Pharmacol. 2011 Nov;80(5):920-9.
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