A-887826
Based on 1 Customer Validation
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.10%
- No. CAS: 1266212-81-0
- Fòrmula: C26H29ClN4O3
- Peso molecular:480.99
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
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Neuroprotective Compound Library
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Sodium Channel Blocker Library
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Membrane Protein-targeted Compound Library
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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
Actividad biológica
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Nav1.8 1.1 nM (IC50) |
A-887826 is approximately 3 fold less potent to block Na(v)1.2, approximately 10 fold less potent to block tetrodotoxin-sensitive sodium (TTX-S Na(+)) currents and is >30 fold less potent to block Na(v)1.5 channels[1].
A-887826 potently blocks tetrodotoxin-resistant sodium (TTX-R Na(+)) currents (IC50=8 nM) from small diameter rat dorsal root ganglion (DRG) neurons in a voltage-dependent fashion[1].
A-887826 effectively suppresses evoked action potential firing when DRG neurons are held at depolarized potentials and reversibly suppresses spontaneous firing in small diameter DRG neurons from complete Freund's adjuvant inflamed rats[1].
A-887826 (100 nM) shifts the mid-point of voltage-dependent inactivation of TTX-R currents by approximately 4mV without affecting voltage-dependent activation and do not exhibit frequency-dependent inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Spraguee Dawley rats (200-300 g)[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration; 1 hour before testing; fourteen days after L5-L6 spinal nerve ligation
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Result:Produced a dose-dependent attenuation of tactile allodynia in this experimental pain model.
Chemical Information
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No. CAS 1266212-81-0
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Appearance Solid
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Peso molecular 480.99
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Fòrmula C26H29ClN4O3
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC=C(OCCCC)C(Cl)=C2)=CN=C1)NCC3=CC=CN=C3N4CCOCC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (519.76 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0790 mL | 10.3952 mL | 20.7905 mL | 51.9761 mL |
| 5 mM | 0.4158 mL | 2.0790 mL | 4.1581 mL | 10.3952 mL | |
| 10 mM | 0.2079 mL | 1.0395 mL | 2.0790 mL | 5.1976 mL | |
| 15 mM | 0.1386 mL | 0.6930 mL | 1.3860 mL | 3.4651 mL | |
| 20 mM | 0.1040 mL | 0.5198 mL | 1.0395 mL | 2.5988 mL | |
| 25 mM | 0.0832 mL | 0.4158 mL | 0.8316 mL | 2.0790 mL | |
| 30 mM | 0.0693 mL | 0.3465 mL | 0.6930 mL | 1.7325 mL | |
| 40 mM | 0.0520 mL | 0.2599 mL | 0.5198 mL | 1.2994 mL | |
| 50 mM | 0.0416 mL | 0.2079 mL | 0.4158 mL | 1.0395 mL | |
| 60 mM | 0.0347 mL | 0.1733 mL | 0.3465 mL | 0.8663 mL | |
| 80 mM | 0.0260 mL | 0.1299 mL | 0.2599 mL | 0.6497 mL | |
| 100 mM | 0.0208 mL | 0.1040 mL | 0.2079 mL | 0.5198 mL |
A-887826 Related Classifications
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