PF-05251749 is a CK1δinhibitor. PF-05251749 demonstrated potent inhibition of CK1δ (IC₅₀ ≈ 4.7 nM) and CK1ε (IC₅₀ ≈ 9.8 nM) enzymatic activity, with good selectivity over other kinases. In animal models, oral administration of PF-05251749 effectively shifted circadian phase timing in a dose-dependent manner and showed favorable pharmacokinetics with high brain-to-plasma ratios.
MedKoo Cat#: 126474
Name: PF-05251749
CAS#: 1383376-92-8
Chemical Formula: C17H12FN3O2
Exact Mass: 309.0914
Molecular Weight: 309.30
Elemental Analysis: C, 66.02; H, 3.91; F, 6.14; N, 13.59; O, 10.35
The following data is based on the product molecular weight 309.30 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
