PF 04671536 hydrochloride

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Cat.No. 6024 - PF 04671536 hydrochloride | C14H18N8OS.HCl | CAS No. 1305116-67-9
Description: Potent and selective PDE8B/8A inhibitor
Chemical Name: 5-Methyl-3-[[(2R)-4-(2-thiazolylmethyl)-2-morpholinyl]methyl]-3H-1,2,3-triazolo[4,5-d]pyrimidin-7-amine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

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
DMSO 38.29 100
water 7.66 20mM with gentle warming

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

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Product Datasheets

Safety Datasheet

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


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Citations for PF 04671536 hydrochloride

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