| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C35H35Cl3F3N7O3S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PF-06456384 trihydrochloride is an extremely potent, selective Nav1.7 sodium channel blocker with IC50 values of 0.01 nM for hNaV1.7, 75 nM for rNaV1.7 and less than 0.1 nM for mNaV1.7, yet it shows no significant analgesic efficacy in the mouse Formalin pain model[1][2]. It is supplied as a white to off-white solid (C35H35Cl3F3N7O3S2, MW 829.18) at 98.41% purity.
Physical & Chemical Properties
| CAS Number | 1834610-75-1 |
|---|---|
| Molecular Formula | C35H35Cl3F3N7O3S2 |
| Molecular Weight | 829.18 g/mol |
| Purity | 98.41% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | N#CC1=CC(S(=O)(NC2=NC=NS2)=O)=CC=C1OC3=CC=C(C4=CC(C(F)(F)F)=CC=C4)C=C3C5=CC(CNCCC6CCNCC6)=NC=C5.[H]Cl.[H]Cl.[H]Cl |
| Target | Nav |
| Signaling Pathway | Membrane Transporter/Ion Channel |
| Solubility | In Vitro: DMSO: 125 mg/mL (150.75 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
h Nav1.7 0.01 nM (IC50) |
rNaV1.7 75 nM (IC50) |
hNav1.1 314 nM (IC50) |
hNav1.2 3 nM (IC50) |
hNav1.3 6438 nM (IC50) |
hNav1.4 1451 nM (IC50) |
hNav1.5 2592 nM (IC50) |
hNav1.6 5.8 nM (IC50) |
hNav1.8 26000 nM (IC50) |
mNaV1.7 <0.1 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 125 mg/mL (150.75 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In the PatchXpress automated electrophysiology assay, PF-06456384 trihydrochloride potently inhibits NaV1.7 channels with an IC50 of 0.58 nM[1]. Human NaV1.7 channels are potently inhibited by PF-06456384 trihydrochloride in the conventional patch clamp electrophysiology assay, with an IC50 of 0.01 nM[1]. Rat NaV1.7 channels are inhibited by PF-06456384 (trihydrochloride) with an IC50 of 75 nM in the conventional patch clamp electrophysiology assay[1].
In Vivo
In the mouse formalin pain model, PF-06456384 (0.28-5.4 mg/kg; i.v.; infusion) trihydrochloride shows no significant analgesic efficacy[1]. In male Wistar-Han rats, PF-06456384 (20 or 40 mg/kg; i.v.) trihydrochloride yields a plasma concentration 40-fold above the predicted value and does not reach steady state by the 2-hour time point[2].
| Animal Model | Wild-type mice[1] |
|---|---|
| Dosage | 0.28 mg/kg; 5.4 mg/kg |
| Administration | i.v.; continuous infusion |
| Result | Achieved an unbound plasma concentration ≥60× the mouse NaV1.7 IC50. Produced no significant reduction in motion counts (pain-related behavior) relative to vehicle control at either dose. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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