产品
编 号：F741324
分子式：C16H16ClN5O3
分子量：361.78
分子式：C16H16ClN5O3
分子量：361.78
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1962178-27-3
产品详情
生物活性：
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.?PF-04802367 shows desirable central nervous system (CNS)?properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50?values of 10.0 and 9.0 nM in mobility shift assays, respectively.
体内研究：
PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels?in vivo.?Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent. PF-04802367 (PF-367), a potent type-I dual GSK-3α/β?inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo.Animal Model:Sprague-Dawley rats
Dosage:1, 3.2, 10, 32 or 50 mg/kg
Administration:A single subcutaneous
Result:Inhibition of phosphorylation of tau in brain is dose-dependent.
体外研究：
PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity?in vitro?with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively.PF-367 has reasonable?in vitro?stability in human hepatic microsomes (t1/2=78.7 min), has excellent passive permeability.In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC50?of 466 nM.PF-367 has good cell viability (IC50?of 117 μM in THLE cytotoxicity assays) and an IC50?>100 μM in a hERG screening assay.PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC50?of 6.2 μM, gene transcription in U20S cells with EC50?of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC50?of 9.0 μM.
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.?PF-04802367 shows desirable central nervous system (CNS)?properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50?values of 10.0 and 9.0 nM in mobility shift assays, respectively.
体内研究：
PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels?in vivo.?Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent. PF-04802367 (PF-367), a potent type-I dual GSK-3α/β?inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo.Animal Model:Sprague-Dawley rats
Dosage:1, 3.2, 10, 32 or 50 mg/kg
Administration:A single subcutaneous
Result:Inhibition of phosphorylation of tau in brain is dose-dependent.
体外研究：
PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity?in vitro?with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively.PF-367 has reasonable?in vitro?stability in human hepatic microsomes (t1/2=78.7 min), has excellent passive permeability.In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC50?of 466 nM.PF-367 has good cell viability (IC50?of 117 μM in THLE cytotoxicity assays) and an IC50?>100 μM in a hERG screening assay.PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC50?of 6.2 μM, gene transcription in U20S cells with EC50?of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC50?of 9.0 μM.
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