PF 05089771
Based on 4 publication(s) in Google Scholar
PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.87%
- CAS 番号: 1235403-62-9
- 分子式: C18H12Cl2FN5O3S2
- 分子量:500.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Anti-diabetic Compound Library
HY-L040
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Orally Active Compound Library
HY-L061
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Neuroprotective Compound Library
HY-L070
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Targeted Diversity Library
HY-L099
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Sodium Channel Blocker Library
HY-L118
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
MedChemExpress（MCE）の使用を引用している文献 PF 05089771
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生物活性
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Nav1.7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
11 nM
Compound: 1b; PF-05089771
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Inhibition of human Nav1.7 expressed in HEK293 cells
Inhibition of human Nav1.7 expressed in HEK293 cells
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[PMID: 28389149] |
| HEK293 | IC50 |
25 μM
Compound: 1b; PF-05089771
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Inhibition of human Nav1.5 expressed in HEK293 cells
Inhibition of human Nav1.5 expressed in HEK293 cells
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[PMID: 28389149] |
| HEK293 | IC50 |
>10 μM
Compound: 1a; PF-05089771
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Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method
Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method
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[PMID: 28465103] |
| HEK293 | IC50 |
11 nM
Compound: 1a; PF-05089771
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Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method
Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method
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[PMID: 28465103] |
| HEK293 | IC50 |
>10 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.011 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.11 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.16 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.85 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
10 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
11 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
25 μM
Compound: 3; PF-05089771
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Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
3.5 μM
Compound: 9; PF-05089771
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Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as suppression of [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition measured after 2 mins by liquid scintillation counting
Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as suppression of [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition measured after 2 mins by liquid scintillation counting
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10.1039/C6MD00190D |
| HEK293-A | IC50 |
>100000 nM
Compound: II
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Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
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[PMID: 32392056] |
| HEK293-A | IC50 |
13 nM
Compound: II
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Inhibition of human NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
Inhibition of human NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
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[PMID: 32392056] |
| HEK293-A | IC50 |
4.9 nM
Compound: II
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Inhibition of mouse NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
Inhibition of mouse NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
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[PMID: 32392056] |
| HEK293-A | IC50 |
>100000 nM
Compound: II
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Inhibition of human NaV1.1/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
Inhibition of human NaV1.1/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method
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[PMID: 32392056] |
PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4)[1].
PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5, Fig 5D) whilst 100 nM resulted in complete block[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1235403-62-9
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性状 Solid
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分子量 500.35
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分子式 C18H12Cl2FN5O3S2
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Color White to off-white
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SMILES
O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Molecular determinant of low-voltage dependence of human Nav1.7 inactivation revealed by efficacy-based Nav1.7 selective inhibitor. [Abstract]2026 Feb 10;17(1):2559. PMID: 41667447 -
Nat Commun
2023 Jun 3;14(1):3224. PMID: 37270609 -
Front Pharmacol
Mechanisms Underlying Gastrodin Alleviating Vincristine-Induced Peripheral Neuropathic Pain. [Abstract]2021 Dec 16:12:744663. PMID: 34975470 -
FEBS J
Transcription factor mesenchyme homeobox protein 2 (MEOX2) modulates nociceptor function. [Abstract]2022 Jun;289(12):3457-3476. PMID: 35029322
溶剤 & 溶解度
DMSO : 100 mg/mL (199.86 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.00 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (4.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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% Tween-80 in Saline
Solubility: 5 mg/mL (9.99 mM); Suspended solution; Need ultrasonic
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.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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]. Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9986 mL | 9.9930 mL | 19.9860 mL | 49.9650 mL |
| 5 mM | 0.3997 mL | 1.9986 mL | 3.9972 mL | 9.9930 mL | |
| 10 mM | 0.1999 mL | 0.9993 mL | 1.9986 mL | 4.9965 mL | |
| 15 mM | 0.1332 mL | 0.6662 mL | 1.3324 mL | 3.3310 mL | |
| 20 mM | 0.0999 mL | 0.4997 mL | 0.9993 mL | 2.4983 mL | |
| 25 mM | 0.0799 mL | 0.3997 mL | 0.7994 mL | 1.9986 mL | |
| 30 mM | 0.0666 mL | 0.3331 mL | 0.6662 mL | 1.6655 mL | |
| 40 mM | 0.0500 mL | 0.2498 mL | 0.4997 mL | 1.2491 mL | |
| 50 mM | 0.0400 mL | 0.1999 mL | 0.3997 mL | 0.9993 mL | |
| 60 mM | 0.0333 mL | 0.1666 mL | 0.3331 mL | 0.8328 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2498 mL | 0.6246 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1999 mL | 0.4997 mL |
PF 05089771 関連分類
HY-12883 関連分類
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