Biological Activity
Potent and selective PDE8B/8A inhibitor ( IC50 values are 1.3 and 1.9 nM, respectively). Exhibits selectivity for PDE8A/B over other PDEs (IC50 values are >10 μM) and a range of other targets. Increases glucose-dependent insulin secretion from human pacreatic islet cells. Orally bioavailable.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc
Technical Data
| M. Wt | 382.87 |
| Formula | C14H18N8OS.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1305116-67-9 |
| InChI Key | KNBIGIZPAKPDTF-HNCPQSOCSA-N |
| Smiles | CC1=NC(N)=C2N=NN(C2=N1)C[C@H]3CN(CCO3)CC4=NC=CS4.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 | |||
| water | 7.66 | 20mM with gentle warming | |
| DMSO | 38.29 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 382.87. 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 |
|---|---|---|---|
| 1 mM | 2.61 mL | 13.06 mL | 26.12 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
DeNinno et al (2012) Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. Bioorg.Med.Chem.Lett. 22 5721 PMID: 22858141
Keywords: PF 04671536 hydrochloride, supplier, PF04671536, hydrochloride, diabetes, phosphodiesterase, 8A, 8B, PDE, potent, selective, orally, bioavailable, antidiabetics, inhibitors, inhibits, Phosphodiesterases, Phosphodiesterases, Tocris Bioscience
