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Product Name:PF-04802367
CAS:1962178-27-3
Purity:>=98% Remarks:Reach out to us for more information about custom solutions.
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Sigma-Aldrich
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| Products Intro: |
Product Name:PF-04802367
CAS:1962178-27-3
Purity:>=98% (HPLC) Package:5MG Remarks:PZ0313-5MG
|
PF-04802367 manufacturers
- PF-04802367
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- $44.00
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2026-06-02
- CAS:1962178-27-3
- Purity: 98.76%
- Supply Ability: 10g
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| | PF-04802367 Basic information |
| Product Name: | PF-04802367 | | Synonyms: | PF-04802367;4-Oxazolecarboxamide, 5-(3-chloro-4-methoxyphenyl)-N-[3-(1H-1,2,4-triazol-1-yl)propyl]-;PF367,PF 367,protein,disease,Alzheimer,PF-04802367,PF-367,Glycogen synthase kinase-3,kinase-3,synthase,Inhibitor,phosphorylation,neurology,GSK-3,neurodegenerative,tau,Glycogen synthase kinase 3,PF04802367,inhibit,Glycogen,PF 04802367;N-(3-(1H-1,2,4-Triazol-1-yl)propyl)-5-(3-chloro-4-methoxyphenyl)oxazole-4-carboxamide;PF-04802367, 10 mM in DMSO;PF-04802367 ，E2819 | | CAS: | 1962178-27-3 | | MF: | C16H16ClN5O3 | | MW: | 361.78 | | EINECS: | | | Product Categories: | | | Mol File: | 1962178-27-3.mol |  |
| | PF-04802367 Chemical Properties |
| storage temp. | -20°C | | solubility | DMSO: 20mg/mL, clear | | form | powder | | color | white to beige | | InChI | 1S/C16H16ClN5O3/c1-24-13-4-3-11(7-12(13)17)15-14(20-10-25-15)16(23)19-5-2-6-22-9-18-8-21-22/h3-4,7-10H,2,5-6H2,1H3,(H,19,23) | | InChIKey | RQFYFNAGNBUGFC-UHFFFAOYSA-N | | SMILES | ClC1=CC(C2=C(C(NCCCN3N=CN=C3)=O)N=CO2)=CC=C1OC |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral |
| | PF-04802367 Usage And Synthesis |
| Uses | 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[1]. | | Biochem/physiol Actions | PF-04802367 is also known as [N-(3-(1H-1,2,4-triazol-1-yl)propyl)-5-(3-chloro-4-methoxyphenyl)oxazole-4-carboxamide) or PF-367. It regulates tau phosphorylation in the brain. | | in vivo | 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[1].
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[2]. | Animal Model: | Sprague-Dawley rats[1] | | 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.
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| | IC 50 | GSK-3α: 10 nM (IC50); GSK-3β: 9 nM (IC50) | | References | [1] Steven H Liang,et al. Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging. Angew Chem Int Ed Engl.2016 Aug 8;55(33):9601-5. DOI:10.1002/anie.201603797
[2] Vadim Bernard-Gauthier, et al. Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery. J Med Chem.2019 Nov 14;62(21):9600-9617. DOI:10.1021/acs.jmedchem.9b01030 |
| | PF-04802367 Preparation Products And Raw materials |
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