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> TAK-715 [303162-79-0]

TAK-715 [303162-79-0]

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Referentie HY-10456-1mL

Formaat : 10mM/1mL

Merk : MedChemExpress


Description

TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model[1][2].

IC50 & Target[1][2]

p38α

7.1 nM (IC50)

p38β

200 nM (IC50)

p38δ

>10 μM (IC50)

p38γ

>10 μM (IC50)

CK1γ2

 

CK1ε

 

Cellular Effect
Cell Line Type Value Description References
THP-1 IC50
48 nM
Compound: 8h
In vitro inhibitory activity against lipopolysaccharide-stimulated release of tumor necrosis factor alpha from human monocytic THP-1 cells
In vitro inhibitory activity against lipopolysaccharide-stimulated release of tumor necrosis factor alpha from human monocytic THP-1 cells
[PMID: 16162000]
In Vitro

TAK-715 (compound 8h) inhibits LPS-stimulated release of TNF-α from THP-1 (IC50=48 nM) and has no inhibitory activity for major CYPs, including CYP3A4. TAK-715 has no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1 (IC50>10 μM of all)[1].
TAK 715 (10 μM; 1 hour) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells[2].
TAK-715 (1 μM; pretreatment for 16 hours) dramatically suppresses Norepinephrine (NE)-stimulated induction of fibronectin, CTGF, and Snai1 expression in TGF-β1-treated HK-2 cells at both the mRNA and protein levels[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAK-715 Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (125.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5031 mL 12.5153 mL 25.0307 mL
5 mM 0.5006 mL 2.5031 mL 5.0061 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
Références

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