DSP-2230
Based on 1 Customer Validation
DSP-2230 is the orally active inhibitor for voltage-gated sodium channel that inhibits Nav1.7-, Nav1.8-, and Nav1.9-derived sodium currents with IC50s of 7.1 μM, 11.4 μM and 6.7 μM, respectively. DSP-2230 can be used to improve neuropathic pain.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.33%
- CAS. Nr.: 1233231-30-5
- Formel: C20H20F3N5O2
- Molecular Weight:419.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
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Biologische Aktivität
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Nav1.9 6.7 μM (IC50) |
Nav1.7 7.1 μM (IC50) |
Nav1.8 11.4 μM (IC50) |
DSP-2230 inhibits Nav1.7, 1.8, and 1.9 sodium channels, reduces the influx of sodium ions, inhibits the generation and propagation of neuronal action potentials, thereby exhibiting analgesic activity[3].
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:C57BL/6 wildtype and R222S mutant mouse[3]
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Dosage:3-30 mg/kg
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Administration:po, once daily for 6 days
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Result:Increased the latency time in hot plate test.
Reduced the nociceptive behaviors in cold plate text.
Chemical Information
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CAS. Nr. 1233231-30-5
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Appearance Solid
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Molecular Weight 419.40
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Formel C20H20F3N5O2
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Color White to off-white
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SMILES
C[C@H](NCC1=NC2=CC=C(OC3=CC(F)=C(F)C(F)=C3)N=C2N1C4CCC4)C(N)=O
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Synonyms
ANP-230
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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 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (238.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.25 mg/mL (5.36 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (5.36 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 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.
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 (273 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]. Bagal SK, et al. Voltage gated sodium channels as drug discovery targets. Channels (Austin). 2015;9(6):360-6. [Content Brief]
[2]. Sara Sabina Hadida-Ruah, et al. Sulfonamides as modulators of sodium channels.
[3]. Okuda H, et al., Reduced pain sensitivity of episodic pain syndrome model mice carrying a Nav1.9 mutation by ANP-230, a novel sodium channel blocker. Heliyon. 2023 Apr 14;9(4):e15423. [Content Brief]
[4]. Kamei T, et al., Unique electrophysiological property of a novel Nav1.7, Nav1.8, and Nav1.9 sodium channel blocker, ANP-230. Biochem Biophys Res Commun. 2024 Aug 20;721:150126. [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 | 2.3844 mL | 11.9218 mL | 23.8436 mL | 59.6090 mL |
| 5 mM | 0.4769 mL | 2.3844 mL | 4.7687 mL | 11.9218 mL | |
| 10 mM | 0.2384 mL | 1.1922 mL | 2.3844 mL | 5.9609 mL | |
| 15 mM | 0.1590 mL | 0.7948 mL | 1.5896 mL | 3.9739 mL | |
| 20 mM | 0.1192 mL | 0.5961 mL | 1.1922 mL | 2.9804 mL | |
| 25 mM | 0.0954 mL | 0.4769 mL | 0.9537 mL | 2.3844 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7948 mL | 1.9870 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5961 mL | 1.4902 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4769 mL | 1.1922 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9935 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7451 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5961 mL |
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