| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PF-04885614 targets the voltage-gated sodium channel NaV1.8, which is primarily expressed in peripheral sensory neurons. By inhibiting NaV1.8, the compound blocks the influx of sodium ions that is essential for the initiation and propagation of action potentials. This inhibition reduces the excitability of nociceptive neurons and attenuates pain signal transmission to the central nervous system. The selectivity of PF-04885614 for NaV1.8 over other sodium channel subtypes makes it a valuable tool for studying the role of this channel in pain and other neurological conditions.
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| ln Vitro |
In vitro, PF-04885614 has been characterized as a potent inhibitor of NaV1.8. The compound's activity has been demonstrated in patch-clamp electrophysiology studies using cells expressing recombinant NaV1.8 channels. PF-04885614 blocks NaV1.8 currents in a concentration-dependent manner, with an IC₅₀ in the low micromolar range. The compound shows selectivity for NaV1.8 over other sodium channel subtypes, which is important for reducing off-target effects.
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| ln Vivo |
In vivo, PF-04885614 has the potential to be developed as a therapeutic agent for pain management. By blocking NaV1.8 in sensory neurons, the compound could attenuate pain signals without affecting other sodium channels involved in essential physiological functions. The compound's potential for the treatment of neurological and neurodevelopmental diseases is also being explored. However, in vivo studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for PF-04885614 involve measuring its inhibition of NaV1.8 sodium channels. The assay is typically performed using patch-clamp electrophysiology on cells expressing recombinant NaV1.8 channels. Whole-cell or voltage-clamp configurations are used to measure sodium currents in the presence of varying concentrations of the compound. The IC₅₀ value is calculated from the concentration-response curve. Selectivity is assessed by testing the compound against a panel of other sodium channel subtypes.
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| Cell Assay |
In vitro cellular experiments for PF-04885614 are performed using cells expressing NaV1.8 channels. The compound's effect on sodium currents is measured using patch-clamp electrophysiology. Alternatively, fluorescence-based membrane potential assays can be used to measure channel activity in a high-throughput format. Cells are loaded with a voltage-sensitive dye, and the change in fluorescence upon channel activation is monitored in the presence of varying concentrations of the compound. The IC₅₀ value is calculated from the concentration-response curve.
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| Animal Protocol |
In vivo animal studies for PF-04885614 would typically involve mouse or rat models of pain. The compound would be administered via intravenous, intraperitoneal, or oral routes. The analgesic efficacy of the compound would be evaluated using behavioral assays such as the hot plate test or the formalin test. The compound's effects on motor function and other neurological parameters would also be assessed. Pharmacokinetic parameters would be evaluated from plasma samples.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of PF-04885614 have not been extensively reported in the literature. As a small molecule with a molecular weight of 285.27 g/mol, it is expected to have reasonable oral bioavailability if formulated appropriately. The compound's lipophilicity and plasma protein binding would influence its distribution and half-life. Metabolism would likely occur in the liver via cytochrome P450 enzymes.
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| Toxicity/Toxicokinetics |
The toxicity profile of PF-04885614 has not been extensively characterized in the literature. As a sodium channel blocker, it is expected to have a targeted mechanism of action with limited off-target effects if it is selective for NaV1.8. However, off-target inhibition of other sodium channels could lead to adverse effects such as cardiac arrhythmias or neurological symptoms. Standard toxicology studies would be required to fully characterize its safety profile.
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| References | |
| Additional Infomation |
PF-04885614 is a potent inhibitor of the sodium channel NaV1.8, which is predominantly expressed in sensory neurons and is implicated in pain signaling. The compound has potential for the treatment of neurological and neurodevelopmental diseases. By blocking NaV1.8, PF-04885614 could attenuate pain signals without affecting other sodium channels involved in essential physiological functions. This compound represents a valuable tool for studying the role of NaV1.8 in pain and other conditions and has potential as a therapeutic agent for pain management.
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| Molecular Formula |
C₁₃H₁₄F₃N₃O
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|---|---|
| Molecular Weight |
285.26
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| Exact Mass |
285.108
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| CAS # |
1480833-70-2
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| PubChem CID |
65459349
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
414.6±45.0 °C at 760 mmHg
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| Flash Point |
204.6±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.527
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| LogP |
3.13
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
327
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(C1=NC=C(N1)C2=CC=C(C=C2)OC(F)(F)F)N
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| InChi Key |
AGORGFNWYAUYSU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14F3N3O/c1-12(2,17)11-18-7-10(19-11)8-3-5-9(6-4-8)20-13(14,15)16/h3-7H,17H2,1-2H3,(H,18,19)
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| Chemical Name |
2-[5-[4-(trifluoromethoxy)phenyl]-1H-imidazol-2-yl]propan-2-amine
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| Synonyms |
PF04885614; PF 04885614
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~876.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5056 mL | 17.5279 mL | 35.0557 mL | |
| 5 mM | 0.7011 mL | 3.5056 mL | 7.0111 mL | |
| 10 mM | 0.3506 mL | 1.7528 mL | 3.5056 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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