PF-04802367

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、高选择性的 GSK-3 抑制剂，在酶测定中对人 GSK-3β 的 IC50 为 2.1 nM。

A potent, highly selective GSK-3 inhibitor with IC50 of 2.1 nM for human GSK-3β in enzyme assays; shows equal effectivity against GSK-3α and GSK-3β with IC50 of 10.0 and 9.0 nM respectively in mobility shift assays, inhibits phosphorylation of tau with an IC50 of 466 nM in a stable inducible CHO cell line over-expressing GSK-3β and substrate tau; modulates tau phosphorylation in?vitro and in?vivo.

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) 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.

PF04802367 | PF 04802367 | PF-367

PI3K/Akt/mTOR signaling

GSK-3

GSK-3

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1962178-27-3

361.786

C16H16ClN5O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (276.41 mM)

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N-(3-(1H-1,2,4-triazol-1-yl)propyl)-5-(3-chloro-4-methoxyphenyl)oxazole-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years