PF-05198007
Based on 1 Customer Validation
PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.27%
- CAS. Nr.: 1235406-19-5
- Formel: C19H12ClF4N5O3S2
- Molecular Weight:533.91
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
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Nav1.7 |
In Vitro
PF-05198007 (30 nM) blocks on average 83.0 ± 2.7% of the total TTX-S current indicating that the major TTX-S conductance is carried through Nav1.7 channels in small-diameter mouse DRG neurons (n = 35)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult Male C57Bl/6J Wild type (WT) and Nav1.7Nav1.8Cre mice[1].
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Dosage:1 or 10 mg/kg.
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Administration:Orally once.
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Result:Reduced the flare response to capsaicin for the duration of the observation period (55 mins; Vehicle; 4930 ± 751 versus 1 and 10 mg/kg 1967 ± 472 and 2265 ± 382, respectively (n = 7), AUC, p < 0.05).
Chemical Information
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CAS. Nr. 1235406-19-5
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Appearance Solid
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Molecular Weight 533.91
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Formel C19H12ClF4N5O3S2
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Color Off-white to light yellow
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SMILES
O=S(C1=CC(Cl)=C(OC2=CC=C(C(F)(F)F)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 150 mg/mL (280.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.75 mg/mL (7.02 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. [Content Brief]
[2]. Kushnarev M, et al. Neuropathic pain: preclinical and early clinical progress with voltage-gated sodium channel blockers. Expert Opin Investig Drugs. 2020 Mar;29(3):259-271. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8730 mL | 9.3649 mL | 18.7297 mL | 46.8244 mL |
| 5 mM | 0.3746 mL | 1.8730 mL | 3.7459 mL | 9.3649 mL | |
| 10 mM | 0.1873 mL | 0.9365 mL | 1.8730 mL | 4.6824 mL | |
| 15 mM | 0.1249 mL | 0.6243 mL | 1.2486 mL | 3.1216 mL | |
| 20 mM | 0.0936 mL | 0.4682 mL | 0.9365 mL | 2.3412 mL | |
| 25 mM | 0.0749 mL | 0.3746 mL | 0.7492 mL | 1.8730 mL | |
| 30 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 40 mM | 0.0468 mL | 0.2341 mL | 0.4682 mL | 1.1706 mL | |
| 50 mM | 0.0375 mL | 0.1873 mL | 0.3746 mL | 0.9365 mL | |
| 60 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL | |
| 80 mM | 0.0234 mL | 0.1171 mL | 0.2341 mL | 0.5853 mL | |
| 100 mM | 0.0187 mL | 0.0936 mL | 0.1873 mL | 0.4682 mL |
PF-05198007 Related Classifications
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