A 33

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Cat.No. 6313 - A 33 | C19H18ClN3O2S | CAS No. 915082-52-9
Description: Potent and selective PDE4B inhibitor
Chemical Name: 2-[4-[[2-(5-Chloro-2-thienyl)-5-ethyl-6-methyl-pyrimidin-4-yl]amino]phenyl]acetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

Potent and selective PDE4B inhibitor (IC50 = 15 nM); exhibits >100-fold selectivity for PDE4B over 4D. Regulates cAMP in inflammatory cells. Inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. Reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. Also exhibits antidepressant-like effects. Orally bioavailable.

Technical Data

M. Wt 387.88
Formula C19H18ClN3O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 915082-52-9
PubChem ID 15951010
InChI Key FDVSPBLZPJMXFV-UHFFFAOYSA-N
Smiles CCC1=C(N=C(C2=CC=C(S2)Cl)N=C1NC3=CC=C(C=C3)CC(O)=O)C

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.79 100

Preparing Stock Solutions

The following data is based on the product molecular weight 387.88. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.58 mL 12.89 mL 25.78 mL
5 mM 0.52 mL 2.58 mL 5.16 mL
10 mM 0.26 mL 1.29 mL 2.58 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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References

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

Naganuma et al (2009) Discovery of selective PDE4B inhibitors. Bioorg.Med.Chem.Lett. 19 3174 PMID: 19447034

Zhang et al (2017) Comparison of the pharmacological profiles of selective PDE4B and PDE4D inhibitors in the central nervous system. Sci.Rep. 7 40115 PMID: 28054669

Wilson et al (2017) Therapeutic benefits of phosphodiesterase 4B inhibition after traumatic brain injury. PLoS One 12 e0178013 PMID: 28542295


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