AS 2444697

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Cat.No. 5430 - AS 2444697 | C19H20N6O4.HCl | CAS No. 1287665-60-4
Description: Potent and selective IRAK4 inhibitor
Chemical Name: N-[3-Aminocarbonyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-2-(2-methyl-4-pyridinyl)-4-oxazolecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor (IC50 = 21 nM). Displays 30-fold selectivity for IRAK4 over IRAK1. Inhibits LPS-induced TNF-α and IL-6 production in PBMCs in vitro. Renoprotective and anti-inflammatory in a rodent model of chronic kidney disease.

Compound Libraries

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Technical Data

M. Wt 432.86
Formula C19H20N6O4.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1287665-60-4
PubChem ID 118719434
InChI Key FGNHLIIFEDYNFZ-UHFFFAOYSA-N
Smiles O=C(N)C2=NN(C=C2NC(C3=COC(C4=CC=NC(C)=C4)=N3)=O)C1CCOCC1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.66 20 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 432.86. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 11.55 mL 57.76 mL 115.51 mL
1 mM 2.31 mL 11.55 mL 23.1 mL
2 mM 1.16 mL 5.78 mL 11.55 mL
10 mM 0.23 mL 1.16 mL 2.31 mL

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References

References are publications that support the biological activity of the product.

Chaudhary (2015) Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders. J.Med.Chem. 58 96 PMID: 25479567

Kondo et al (2014) Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch.Pharmacol. 387 909 PMID: 25052043

Schmaderer and Heemann (2014) Blocking innate immunity to slow the progression of chronic kidney disease. Naunyn Schmiedebergs Arch.Pharmacol. 387 905 PMID: 25107563


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Keywords: AS 2444697, AS 2444697 supplier, AS2444697, potent, selective, interleukin-1, receptor-associated, kinase, 4, IRAK4, inhibitors, inhibits, anti-inflammatory, renoprotective, Cytokines, IRAK, 5430, Tocris Bioscience

Citations for AS 2444697

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