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    TAK-715
    TAK-715

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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 #: V0487
    CAS #: 303162-79-0Purity ≥98%

    Description: TAK-715 is a novel, potent and selective p38 MAPK (p38 mitogen-activated protein) inhibitor with potential anti-inflammatory activity. It inhibits p38α with an IC50 of 7.1 nM, and is 28-fold more selective for p38α over p38β, it shows no/little inhibition against p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. TAK-715 is currently under clinical investigation for the treatment of Rheumatoid arthritis-RA. 

    References: J Med Chem. 2005 Sep 22;48(19):5966-79; Chem Biol. 2011 Apr 22;18(4):485-94.

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    Molecular Weight (MW)399.51
    FormulaC24H21N3OS
    CAS No.303162-79-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (200.2 mM)
    Water: <1 mg/mL
    Ethanol: 16 mg/mL (40.0 mM)
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    Synonyms

    Synonym: TAK 715, TAK715, TAK-715

    Chemical Name: N-(4-(2-ethyl-4-(m-tolyl)thiazol-5-yl)pyridin-2-yl)benzamide

    InChi Key: HEKAIDKUDLCBRU-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H21N3OS/c1-3-21-27-22(18-11-7-8-16(2)14-18)23(29-21)19-12-13-25-20(15-19)26-24(28)17-9-5-4-6-10-17/h4-15H,3H2,1-2H3,(H,25,26,28)

    SMILES Code: O=C(NC1=NC=CC(C2=C(C3=CC=CC(C)=C3)N=C(CC)S2)=C1)C4=CC=CC=C4 


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    In Vitro

    In vitro activity: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop.


    Kinase Assay: TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. 


    Cell Assay: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop.

    In VivoTAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model.
    Animal modelAdjuvant-induced arthritis (AA) rat model
    Formulation & DosageDissolved in saline; 30 mg/kg; p.o.
    ReferencesJ Med Chem. 2005 Sep 22;48(19):5966-79; Chem Biol. 2011 Apr 22;18(4):485-94.


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

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