2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. LTGO-33

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.

For research use only. We do not sell to patients.

LTGO-33 Chemical Structure

LTGO-33 Chemical Structure

CAS No. : 2834106-06-6

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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1].

IC50 & Target

hNav1.8

 

In Vitro

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.
Molecular Weight

467.44

Formula

C21H17F4N3O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1393 mL 10.6966 mL 21.3931 mL
5 mM 0.4279 mL 2.1393 mL 4.2786 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (10.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
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 2.1393 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
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LTGO-33 Related Classifications

Keywords:

LTGO-332834106-06-6LTGO33LTGO 33Sodium ChannelNa channelsNa+ channelspain disordersVSDIIcynomolgus monkeyDRG neuronsInhibitorinhibitorinhibit

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