LTGO-33 |
Catalog No.GC73761
One-Click Copy Product Info
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LTGO-33 est un inhibiteur puissant et sélectif du canal de sodium NaV1.8 voltage-gated.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2834106-06-6
Sample solution is provided at 25 µL, 10mM.
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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.
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].
References:
[1]. Gilchrist JM, et al. Pharmacologic Characterization of LTGO-33, a Selective Small Molecule Inhibitor of the Voltage-Gated Sodium Channel NaV1.8 with a Unique Mechanism of Action. Mol Pharmacol. 2024 Feb 15;105(3):233-249.
| Cas No. | 2834106-06-6 | SDF | |
| Formula | C21H17F4N3O3S | M.Wt | 467.44 |
| Solubility | Storage | -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1393 mL | 10.6966 mL | 21.3931 mL |
| 5 mM | 427.9 μL | 2.1393 mL | 4.2786 mL |
| 10 mM | 213.9 μL | 1.0697 mL | 2.1393 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)