{"product_id":"m33497","title":"PF-04802367","description":"\u003cp style=\"padding-left:1em;\"\u003eF-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.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 1962178-27-3\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 361.78\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C16H16ClN5O3\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e 4-(3-chloro-4-methoxyphenyl)-N-[3-(1H-1, 2, 4-triazol-1-yl)propyl]-1, 3-oxazole-5-carboxamide\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e COC1=CC=C(C=C1Cl)C1N=COC=1C(=O)NCCCN1C=NC=N1\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e VQZHXGWCLUVZQI-UHFFFAOYSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C16H16ClN5O3\/c1-24-13-4-3-11(7-12(13)17)14-15(25-10-20-14)16(23)19-5-2-6-22-9-18-8-21-22\/h3-4,7-10H,2,5-6H2,1H3,(H,19,23)\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSolubility:\u003c\/strong\u003e To be determined\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003ePF-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 \u0026gt;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.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003ePF-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.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eReferences:\u003c\/strong\u003e\u003c\/p\u003e\u003col style=\"padding-left:1em;\"\u003e\n\u003cli\u003eVadim 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.\u003c\/li\u003e\n\u003cli\u003eSteven 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.\u003c\/li\u003e\n\u003c\/ol\u003e\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M33497-2 \/ 2 mg solid","offer_id":39849228894347,"sku":"","price":160.0,"currency_code":"USD","in_stock":true},{"title":"M33497-10 \/ 10 mg solid","offer_id":39849228927115,"sku":"","price":505.0,"currency_code":"USD","in_stock":true},{"title":"M33497-100 \/ 100 mg solid","offer_id":39849228959883,"sku":"","price":3505.0,"currency_code":"USD","in_stock":true},{"title":"M33497-C \/ Contact sales@xcessbio.com for quotation","offer_id":39849228992651,"sku":"","price":100.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/products\/M33497_1643247935.gif?v=1735786032","url":"https:\/\/www.xcessbio.com\/products\/m33497","provider":"Xcess Biosciences","version":"1.0","type":"link"}