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    CAY10505
    CAY10505

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0139
    CAS #: 1218777-13-9Purity ≥98%

    Description: CAY10505, the dehydroxylated form of AS-252424, is a novel, potent and selective inhibitor of PI3Kγ (phosphoinositide 3-kinase) with a potential to improve hypertension-associated vascular endothelial dysfunction. 

    References: Can J Physiol Pharmacol. 2012 Jul;90(7):881-5.

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    Molecular Weight (MW)

    289.28

    Formula

    C14H8FNO3S

    CAS No.

    1218777-13-9

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 58 mg/mL (200.5 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Other info

    Synonym: CAY 10505; CAY10505; CAY-10505

    InChi Key: UFBTYTGRUBUUIL-KPKJPENVSA-N

    InChi Code: InChI=1S/C14H8FNO3S/c15-9-3-1-8(2-4-9)11-6-5-10(19-11)7-12-13(17)16-14(18)20-12/h1-7H,(H,16,17,18)/b12-7+

    SMILES Code: O=C(NC/1=O)SC1=C\C2=CC=C(C3=CC=C(F)C=C3)O2

    Chemical Name

    (E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione


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      This equation is commonly abbreviated as: C1V1 = C2V2

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    In VitroIn Vitro Assay: A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM).

    Cell Assay: In neurons treated with 3.5 μM BA, 200 nM CAY10505 partially reduced the baicalein-induced Akt phosphorylation.

    In VivoIn hypertensive rats, CAY10505 at 0.6 mg.kg-1 p.o. exhibited the following effects 1) effectively reduced MABP; 2) significantly ameliorated vascular endothelium dysfunction in hypertensive rats in combination of DOCA; 3) prominently increased serum nitrite and/or nitrate concentrations.4) prevented hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation.
    Animal modelWistar albino rats
    Formulation & DosageWistar albino rats (180-240 g) of either sex are employed in the present study. For each group, the number of rats used (n) is 6. Group I (normal control): Rats are maintained on a diet of normal chow with drinking water. Group II (hypertensive control): Rats are unilaterally nephrectomized (uninephrectomised) and DOCA (40 mg/kg) is administered by subcutaneous injection (s.c.) twice weekly for 6 weeks, and then the untreated drinking water is replaced with a 1% NaCl solution. Group III (hypertensive rats): Rats are treated with CAY10505 (0.6 mg/kg, per os (p.o)) for 1 week after 5 weeks of treatment with DOCA. Group IV (hypertensive rats): Rats are treated with Losartan (25 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA. Group V (hypertensive rats): Rats are treated with Atorvastatin (30 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA. 
    References[1] Can J Physiol Pharmacol. 2012 Jul;90(7):881-5;   [2] PLoS One.  2013 Jul 19;8(7):e69019.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    CAY10505

    Effects of PI3K inhibitors on the baicalein–activated HIF1α and Epo/VEGF gene transcription in neurons. Neurons were treated with 3.5 μM BA with or without 1 h pretreatment with the pan PI3K inhibitor LY294002 (LY, 10 μM), PI3Kα/β inhibitor (PI3K α inhibitor-2, 50 nM), or PI3Kγ inhibitor (CAY10505, 200 nM). PLoS One, 2013, 8(7):e69019.




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