PRX-2904
PRX-2904 is an orally effective and selective KNa1.1 (KCNT1/Slack/Slo2.2) inhibitor with an IC50 of 40 nM against human KNa1.1-WT. PRX-2904 reduces abnormal neuronal firing in KCNT1 gain-of-function (GoF) models by inhibiting KNa1.1 channel activity. PRX-2904 is useful for research on epilepsy associated with KCNT1 gain-of-function variants.
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- Purity : 99.29%
- CAS No.: 2540502-26-7
- 화학식: C16H12F6N6O2
- 분자량:434.30
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
PRX-2904 inhibits multiple human KCNT1 GoF variants, with IC50 values ranging from 221-1768 nM, among which the IC50 values for G288S and F346L are 221 nM and 1768 nM, respectively[1].
In a binding displacement screen against 80 potential secondary targets, PRX-2904 (10 μM) shows >50% activity only at TSPO and the GABAA Cl− channel, with displacement rates of 63% and 74%, respectively; meanwhile, its IC50 values for hERG, hNaV1.5, CaV1.2, IKs, BK, and KNa1.2 are 11.9, 42, 10.7, 18.5, 13.2, and 16.4 μM, respectively, supporting its good selectivity for KNa1.1[1].
PRX-2904 (1, 10 μM) does not reduce action potential firing at 1 μM, whereas 10 μM decreases the total number of action potentials from 284.4 to 223.4 in CA1 pyramidal neurons of acute brain slices from P16-30 Kcnt1L/L mice; in WT mouse brain slices, neither 1 μM nor 10 μM markedly alters total action potential firing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PRX-2904 (10-150 mg/kg) does not significantly affect spontaneous locomotor distance in WT CD-1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kcnt1L/L (homozygous for mKcnt1-P905L, aged P32−40)[1]
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Dosage:30 mg/kg
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Administration:s.c.; single dose
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Result:Robustly reduced interictal spike frequency that persisted over the 24 h period.
Completely eliminated seizures over the 24 h period.
Achieved a maximum free brain concentration of approximately 270 nM.
Chemical Information
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CAS No. 2540502-26-7
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Appearance Solid
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분자량 434.30
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화학식 C16H12F6N6O2
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Color White to off-white
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SMILES
CN1C(C(N[C@@H](C)C2=NC(C3=CC(C(F)(F)F)=NC=C3)=NO2)=O)=CC(C(F)(F)F)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 200 mg/mL (460.51 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)
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: ≥ 5 mg/mL (11.51 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
순도&문서
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Data Sheet (283 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)
References
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 | 2.3026 mL | 11.5128 mL | 23.0256 mL | 57.5639 mL |
| 5 mM | 0.4605 mL | 2.3026 mL | 4.6051 mL | 11.5128 mL | |
| 10 mM | 0.2303 mL | 1.1513 mL | 2.3026 mL | 5.7564 mL | |
| 15 mM | 0.1535 mL | 0.7675 mL | 1.5350 mL | 3.8376 mL | |
| 20 mM | 0.1151 mL | 0.5756 mL | 1.1513 mL | 2.8782 mL | |
| 25 mM | 0.0921 mL | 0.4605 mL | 0.9210 mL | 2.3026 mL | |
| 30 mM | 0.0768 mL | 0.3838 mL | 0.7675 mL | 1.9188 mL | |
| 40 mM | 0.0576 mL | 0.2878 mL | 0.5756 mL | 1.4391 mL | |
| 50 mM | 0.0461 mL | 0.2303 mL | 0.4605 mL | 1.1513 mL | |
| 60 mM | 0.0384 mL | 0.1919 mL | 0.3838 mL | 0.9594 mL | |
| 80 mM | 0.0288 mL | 0.1439 mL | 0.2878 mL | 0.7195 mL | |
| 100 mM | 0.0230 mL | 0.1151 mL | 0.2303 mL | 0.5756 mL |
PRX-2904 Related Classifications
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