PF 05089771 | Nav1.7 Inhibitor - MedChemExpress
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- PF 05089771
Solubility
In Vivo Dissolution Calculator
Help & FAQs
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.
For research use only. We do not sell to patients.
PF 05089771 Chemical Structure
CAS No. : 1235403-62-9
| Size | Price | Stock | Quantity |
|---|---|---|---|
| Free Sample (0.1 - 0.2 mg) | Apply Now | ||
| Solid + Solvent (Highly Recommended) | |||
| 10 mM * 1 mL in DMSO ready for reconstitution | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| Solution | |||
| 10 mM * 1 mL in DMSO | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| Solid | |||
| 5 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 10 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 25 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 50 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 100 mg | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 | |
| 200 mg | Get quote | ||
| 500 mg | Get quote | ||
* Please select Quantity before adding items.
This product is a controlled substance and not for sale in your territory.
Customer Review
Based on 3 publication(s) in Google Scholar
Other Forms of PF 05089771:
- PF 05089771 tosylate Get quote
PF 05089771 Related Antibodies
3 Publications Citing Use of MCE PF 05089771
- •Nat Commun. 2023 Jun 3;14(1):3224. [Abstract]
- •Front Pharmacol. 2021 Dec 16:12:744663.
- •FEBS J. 2022 Jun;289(12):3457-3476. [Abstract]
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•Related Small Molecules:
•Related Proteins:
View All Sodium Channel Isoform Specific Products:
View All Isoforms Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9Biological Activity
Purity & Documentation
References
Customer Review
| Description | 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[1][2]. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| IC50 & Target |
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| Cellular Effect |
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| In Vitro | 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. PF 05089771 Related Antibodies | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Clinical Trial | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Molecular Weight | 500.35 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Formula | C18H12Cl2FN5O3S2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| CAS No. | 1235403-62-9 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Appearance | Solid | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Color | White to off-white | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| SMILES | O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Shipping | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Storage |
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| Solvent & Solubility | In Vitro: 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) Preparing Stock Solutions
* 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Mass kg g mg μg ng pg = Concentration M mM μM nM pM × Volume L mL μL × Molecular Weight *Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 Concentration (start) M mM μM nM pMC1 × Volume (start) L mL μLV1 = Concentration (final) M mM μM nM pMC2 × Volume (final) L mL μLV2 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.
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.
Dosage mg/kgAnimal weight (per animal) gDosing volume (per animal) μLNumber of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Please enter your animal formula composition: % DMSO + % + % Tween-80 + % Saline Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak. 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). Calculation results: Working solution concentration: mg/mL Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL). The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE). Tel: 609-228-6898 E-mail: [email protected] Technical Support: [email protected] Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline. Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution If the continuous dosing period exceeds half a month, please choose this protocol carefully. 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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Purity & Documentation | Purity: 99.87% Select Batch: HY-12883-591813 HY-12883-614750 HY-12883-17173 HY-12883-40359 HY-12883-426589 HY-12883-21819 HY-12883-586534 HY-12883-603061 Data Sheet (278 KB) SDS (393 KB)COA (254 KB) HNMR (297 KB) RP-HPLC (257 KB) LCMS (116 KB) Handling Instructions (2659 KB) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| References |
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[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.
[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.
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 |
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PF 05089771 Related Classifications
- Disease Areas
- Metabolic or Endocrine Disease Neurological, Eye or Ear Disease
- Glucose Metabolism
- Neurological Disease
- Membrane Transporter/Ion Channel
- Sodium Channel
- Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
PF 050897711235403-62-9PF05089771PF-05089771Sodium ChannelNa channelsNa+ channelspaindiabeticneuropathytetrodotoxinTTX-RInhibitorinhibitorinhibit
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