PF 04671536 hydrochloride

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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)

Biological Activity for PF 04671536 hydrochloride

PF 04671536 hydrochloride is a 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

Compound Libraries for PF 04671536 hydrochloride

PF 04671536 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PF 04671536 hydrochloride

M. Wt 382.87
Formula C14H18N8OS.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1305116-67-9
PubChem ID 131954582
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.

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

Solubility Data for PF 04671536 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 7.66 20 with gentle warming
DMSO 38.29 100

Preparing Stock Solutions for PF 04671536 hydrochloride

The following data is based on the product molecular weight 382.87. 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.

Select a batch to recalculate based on the batch molecular weight:
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 for PF 04671536 hydrochloride

References for PF 04671536 hydrochloride

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

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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