[CAS NO. 1235397-05-3] PF-04856264
PRODUCTS SPECIFICATIONS [1235397-05-3]
DESCRIPTION [1235397-05-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 437.49 |
| Molecular Formula | C20H15N5O3S2 |
| SMILES | O=S(C1=CC=C(OC2=CC=CC=C2C3=CC=NN3C)C(C#N)=C1)(NC4=NC=CS4)=O |
Summary
IC50 & Target
IC50: 28 (human Nav1.7), 131 nM (mouse Nav1.7), 19 nM (cynomolgus monkey Nav1.7), 42 nM (dog Nav1.7) [1]
In Vivo
PF-04856264 (3-30 mg/kg; i.p.) reverses OD1-induced pain behaviors [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 6-8 weeks adult male C57BL/6J mice (OD1-induced spontaneous pain model) [2] |
| Dosage: | 3, 30 mg/kg |
| Administration: | I.p. |
| Result: | Significantly reduced spontaneous pain behaviors in mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 571.44 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2858 mL | 11.4288 mL | 22.8577 mL |
| 5 mM | 0.4572 mL | 2.2858 mL | 4.5715 mL |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2858 mL |
References
- [1] McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc Natl Acad Sci U S A. 2013;110(29):E2724-E2732.
- [2] Deuis JR, et al. Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain. Toxins (Basel). 2016;8(3):78. Published 2016 Mar 17.
