| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PF-05241328 targets Nav1.7 (voltage-gated sodium channel alpha subunit Nav1.7, encoded by the SCN9A gene), a sodium channel that is predominantly expressed in peripheral sensory neurons and sympathetic neurons. Nav1.7 plays a critical role in pain signaling by generating and propagating action potentials in nociceptive neurons. Gain-of-function mutations in Nav1.7 are associated with inherited pain syndromes such as erythromelalgia, while loss-of-function mutations result in congenital insensitivity to pain. PF-05241328 is a potent and selective inhibitor of Nav1.7 with an IC50 of 31 nM. By blocking Nav1.7 channels, PF-05241328 reduces neuronal excitability and pain signal transmission.
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| ln Vitro |
PF-05241328 demonstrates potent in vitro activity as a Nav1.7 inhibitor. The compound has an IC50 of 31 nM for human Nav1.7. PF-05241328 is a selective inhibitor of Nav1.7 over other voltage-gated sodium channel subtypes. The compound's potent and selective Nav1.7 inhibition makes it a valuable tool for studying the role of Nav1.7 in pain signaling and for evaluating Nav1.7 inhibitors as potential analgesics. Detailed electrophysiological data, including effects on channel gating and use-dependent inhibition, are available in the primary literature.
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| ln Vivo |
PF-05241328 has been investigated for the treatment of pain and reached Phase 1 clinical trials. The compound's potent Nav1.7 inhibition and selectivity over other sodium channel subtypes support its potential utility as a non-opioid analgesic. PF-05241328's development for pain indications highlights the therapeutic potential of Nav1.7 inhibitors. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature and clinical trial reports. PF-05241328 is a valuable tool for studying Nav1.7 as a pain target.
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| Enzyme Assay |
The in vitro electrophysiological assay for PF-05241328 measures the inhibition of Nav1.7 sodium channel currents. Cells expressing recombinant human Nav1.7 channels (e.g., HEK293 cells) are patch-clamped in whole-cell configuration. Varying concentrations of PF-05241328 (typically ranging from nanomolar to micromolar) are applied to the cells, and sodium currents are elicited by voltage steps. The inhibition of peak sodium current is measured, and IC50 values are determined by fitting dose-response curves to the inhibition data (31 nM). The compound is dissolved in DMSO and diluted in extracellular recording solution. Selectivity is assessed by testing the compound against other sodium channel subtypes (Nav1.1, Nav1.2, Nav1.3, Nav1.5, Nav1.6, Nav1.8). Appropriate positive controls and negative controls are included in each assay run.
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| Cell Assay |
The in vitro cellular assay for PF-05241328 is performed using cells expressing Nav1.7 channels. Cells are cultured in appropriate medium and loaded with a voltage-sensitive dye or a sodium-sensitive fluorescent indicator. Cells are treated with varying concentrations of PF-05241328 or vehicle control (DMSO), and sodium channel activity is measured by monitoring changes in membrane potential or intracellular sodium levels in response to depolarizing stimuli. The inhibition of sodium channel activity is quantified, and IC50 values are determined. Alternatively, automated patch-clamp systems can be used for higher-throughput screening of sodium channel inhibition.
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| Animal Protocol |
In vivo animal experiments with PF-05241328 are conducted using rodent models of pain, such as the formalin test, hot plate test, or neuropathic pain models. PF-05241328 is administered via oral gavage, intraperitoneal injection, or subcutaneous injection at various doses. Pain responses are measured at specified time points after compound administration. The compound's antinociceptive effects are compared to vehicle-treated controls and to reference analgesics. PF-05241328 reached Phase 1 clinical trials for pain. Detailed experimental protocols, including dosing regimens and endpoints, are described in the primary literature and clinical trial reports.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for PF-05241328 are not extensively documented in publicly available sources. PF-05241328 has a molecular weight of 436.91 and a chemical formula of C19H21ClN4O4S. The compound is soluble in DMSO for formulation purposes. For in vivo administration, the compound is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for PF-05241328 are not extensively documented in publicly available sources. As a research-grade compound, PF-05241328 is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. PF-05241328 reached Phase 1 clinical trials, indicating that some toxicological data are available from clinical studies. Comprehensive toxicological profiling is not available from the current search results.
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| References | |
| Additional Infomation |
PF-05241328 is being studied in the clinical trial NCT01165736 (to calculate the pharmacokinetics (concentration and excretion rate of the compound in the blood) after taking a very low dose of the compound without producing any pharmacological activity).
PF-05241328 is a research compound developed for studying the role of Nav1.7 in pain signaling and for evaluating Nav1.7 inhibitors as non-opioid analgesics. The compound is a potent and selective inhibitor of human Nav1.7 with an IC50 of 31 nM. PF-05241328 has been investigated for the treatment of pain and reached Phase 1 clinical trials. PF-05241328 is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical pain research. PF-05241328 is available from various chemical suppliers for research purposes. Its utility lies in its ability to selectively inhibit Nav1.7 and probe its role in pain signaling. |
| Molecular Formula |
C19H21CLN4O4S
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| Molecular Weight |
436.912441968918
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| Exact Mass |
436.097
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| CAS # |
1387633-03-5
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| PubChem CID |
68109743
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.645
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| LogP |
3.97
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
686
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RVTSXVZXEGFIPW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21ClN4O4S/c1-11(2)10-28-19-16(20)8-14(9-21-19)24-17-6-5-13(7-15(17)12(3)22-24)18(25)23-29(4,26)27/h5-9,11H,10H2,1-4H3,(H,23,25)
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| Chemical Name |
1-(5-Chloro-6-(2-methylpropoxy)-3-pyridinyl)-3-methyl-N-(methylsulfonyl)-1H-indazole-5-carboxamide
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| Synonyms |
PF-05241328; PF 05241328; PF05241328; PF-5241328; PF 5241328; PF5241328.
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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 : ~100 mg/mL (~228.88 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2888 mL | 11.4440 mL | 22.8880 mL | |
| 5 mM | 0.4578 mL | 2.2888 mL | 4.5776 mL | |
| 10 mM | 0.2289 mL | 1.1444 mL | 2.2888 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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