Biological Activity
Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 651.47 |
| Formula | C27H41F2N5O.HBr |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1962925-29-6 |
| PubChem ID | 121513889 |
| InChI Key | LXEYYZYDWLAIPW-KBVFCZPLSA-N |
| Smiles | O=C(NC3=CN(C(C)(C)CNCC(C)(C)C)C=N3)[C@H](CCC)N[C@H]2CCC1=CC(F)=CC(F)=C1C2.Br.Br |
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 | 65.15 | 100 | |
| water | 6.51 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 651.47. 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 | 1.53 mL | 7.67 mL | 15.35 mL |
| 5 mM | 0.31 mL | 1.53 mL | 3.07 mL |
| 10 mM | 0.15 mL | 0.77 mL | 1.53 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID: 20363853
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