LTGO-33
Based on 1 Customer Validation
LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research.
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- Pureza: 98.83%
- No. CAS: 2834106-06-6
- Fòrmula: C21H17F4N3O3S
- Peso molecular:467.44
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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hNav1.8 |
LTGO-33 exhibits an IC50 of 33 nM from the closed state and 24 nM from an inactivated state[1].
LTGO-33 displays species specificity for primate NaV1.8 over dog and rodent NaV1.8 and inhibits action potential firing in human dorsal root ganglia neurons[1].
LTGO-33 inhibits TTX-R currents in primary DRG neurons from human (male donors: IC50 of 110 nM, 95% CI: 92 to 120 nM, n = 3-15 neurons per concentration; female donors: IC50 of 120 nM, 95% CI: 100 to 140 nM, 4- 6 neurons per concentration) and cynomolgus monkey (IC50 of 100 nM, 95% CI: 71 to 150 nM, n = 6 cells) but is markedly less effective on DRG neurons from dog (IC50 >10 µM, n = 6 cells), rat (IC50 >30 µM, n = 7 cells), and mouse (IC50 >30 µM, n = 8 cells)[1].
LTGO-33 stabilizs the deactivated state of VSDII, effectively keeping the channel closed by preventing movement of VSDII[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2834106-06-6
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Appearance Solid
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Peso molecular 467.44
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Fòrmula C21H17F4N3O3S
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Color Off-white to light yellow
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SMILES
FC1=CC(C)=C(OC2=NC=C(C=C2C(NC3=CC=CC([S@](=O)(C)=N)=C3)=O)C(F)(F)F)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (213.93 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: ≥ 5 mg/mL (10.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
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.
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 (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.1393 mL | 10.6966 mL | 21.3931 mL | 53.4828 mL |
| 5 mM | 0.4279 mL | 2.1393 mL | 4.2786 mL | 10.6966 mL | |
| 10 mM | 0.2139 mL | 1.0697 mL | 2.1393 mL | 5.3483 mL | |
| 15 mM | 0.1426 mL | 0.7131 mL | 1.4262 mL | 3.5655 mL | |
| 20 mM | 0.1070 mL | 0.5348 mL | 1.0697 mL | 2.6741 mL | |
| 25 mM | 0.0856 mL | 0.4279 mL | 0.8557 mL | 2.1393 mL | |
| 30 mM | 0.0713 mL | 0.3566 mL | 0.7131 mL | 1.7828 mL | |
| 40 mM | 0.0535 mL | 0.2674 mL | 0.5348 mL | 1.3371 mL | |
| 50 mM | 0.0428 mL | 0.2139 mL | 0.4279 mL | 1.0697 mL | |
| 60 mM | 0.0357 mL | 0.1783 mL | 0.3566 mL | 0.8914 mL | |
| 80 mM | 0.0267 mL | 0.1337 mL | 0.2674 mL | 0.6685 mL | |
| 100 mM | 0.0214 mL | 0.1070 mL | 0.2139 mL | 0.5348 mL |
LTGO-33 Related Classifications
HY-157802 Related Classifications
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