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| Targets |
PF-5198007 targets the voltage-gated sodium channel Nav1.7 as a selective antagonist. It exerts its effects by selectively inhibiting the Nav1.7 channel, preventing the influx of sodium ions essential for action potential initiation and propagation in nociceptive neurons. This inhibition modulates pain signaling. In vitro, PF-05198007 (30 nM) inhibits 83.0 ± 2.7% of total TTX-S current in small-diameter mouse DRG neurons.
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| ln Vitro |
PF-05198007 (30 nM) inhibited 83.0 ± 2.7% of the total TTX-S current on average, suggesting that Nav1.7 channels in small-diameter mouse DRG neurons account for the majority of TTX-S conductance (n = 35).[1].
In vitro, PF-5198007 (PF-05198007) at 30 nM inhibits 83.0 ± 2.7% of the total TTX-S current in small-diameter mouse DRG neurons, suggesting Nav1.7 channels account for the majority of TTX-S conductance. The compound is a potent, orally active, and selective arylsulfonamide Nav1.7 inhibitor. |
| ln Vivo |
PF-05198007 (1 or 10 mg/kg, orally) decreases the capsaicin flare response in WT mice, but not in Nav1.7Nav1.8Cre mice [1].
In vivo activity data for PF-5198007 are not extensively detailed in the available literature. The compound is a potent, orally active Nav1.7 inhibitor. It has been studied in animal models of pain, including the mouse capsaicin-induced neurogenic flare model. Specific in vivo efficacy data are limited in the available sources. |
| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PF-5198007 involve voltage-gated sodium channel inhibition assays. The compound's selectivity for Nav1.7 is confirmed using patch-clamp electrophysiology on cells expressing recombinant Nav channels. Inhibition of TTX-S current is measured in DRG neurons.
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| Cell Assay |
In vitro cell-based assays for PF-5198007 use small-diameter mouse DRG neurons. Patch-clamp electrophysiology is employed to measure inhibition of TTX-S sodium currents, with 30 nM inhibiting 83.0 ± 2.7% of total TTX-S current. Selectivity for Nav1.7 over other Nav channels is confirmed through these assays.
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| Animal Protocol |
Animal/Disease Models: Adult male C57Bl/6J wild-type (WT) and Nav1.7Nav1.8Cre mice [1].
Doses: 1 or 10 mg/kg. Doses: Take once orally. Experimental Results: During the observation period (55 min; vehicle; 4930 ± 751 vs. 1967 ± 472 and 2265 ± 382 for 1 and 10 mg/kg, respectively (n = 7), AUC, p < 0.05). In vivo animal studies for PF-5198007 have been conducted in mouse pain models. The compound demonstrates efficacy in the mouse capsaicin-induced neurogenic flare model. Somatic pain behaviors and tibial nerve activity in response to noxious thermal stimulation have been evaluated in Nav1.7Nav1.8 and littermate mice. |
| ADME/Pharmacokinetics |
PF-5198007 has a molecular formula of C19H12ClF4N5O3S2 and a molecular weight of 533.9 g/mol. The IUPAC name is 4-(2-(3-Amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide. The compound is orally active. Storage: dry, dark, at 0-4°C for short term or -20°C for long term.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PF-5198007 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As a Nav1.7 antagonist, potential toxicities would relate to effects on pain perception and sensory neuronal function, though formal toxicological profiles are not reported.
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| References |
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| Additional Infomation |
PF-5198007 (CAS 1235406-19-5) is a selective NaV1.7 antagonist and a potent, orally active arylsulfonamide Nav1.7 inhibitor. At 30 nM, it inhibits 83% of TTX-S current in mouse DRG neurons. The compound shows efficacy in the mouse capsaicin-induced neurogenic flare model. No clinical trial data are available.
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| Molecular Formula |
C19H12CLF4N5O3S2
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|---|---|
| Molecular Weight |
533.906893730164
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| Exact Mass |
533
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| CAS # |
1235406-19-5
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| PubChem CID |
46841789
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
808
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=C(C(=CC=1OC1=CC=C(C(F)(F)F)C=C1C1C=NNC=1N)F)S(NC1=CSC=N1)(=O)=O
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| InChi Key |
QCDLGAPJZJODRJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H12ClF4N5O3S2/c20-12-4-16(34(30,31)29-17-7-33-8-26-17)13(21)5-15(12)32-14-2-1-9(19(22,23)24)3-10(14)11-6-27-28-18(11)25/h1-8,29H,(H3,25,27,28)
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| Chemical Name |
4-[2-(5-amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide
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| Synonyms |
PF5198007; PF 5198007; PF-5198007
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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 : ~150 mg/mL (~280.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (7.02 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 37.5 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: ≥ 3.75 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 37.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8730 mL | 9.3649 mL | 18.7297 mL | |
| 5 mM | 0.3746 mL | 1.8730 mL | 3.7459 mL | |
| 10 mM | 0.1873 mL | 0.9365 mL | 1.8730 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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