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Suzetrigine

(Synonyms: VX-548) Copy Product Info
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Synonyms: VX-548

Catalog No. T69552 Copy Product Info
Purity: 99.87%
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Suzetrigine (VX-548) is a small molecule inhibitor and a highly selective inhibitor of the NaV1.8 target, with oral activity and good peripheral nerve selectivity. Suzetrigine is used for the treatment of moderate to severe acute pain following abdominoplasty or bunionectomy.
Suzetrigine
Cas No. 2649467-58-1
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$53In StockIn Stock
5 mg$116In StockIn Stock
10 mg$173In StockIn Stock
25 mg$281In StockIn Stock
50 mg$482In StockIn Stock
100 mg$786In StockIn Stock
200 mg$1,080In StockIn Stock
1 mL x 10 mM (in DMSO)$120In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.87%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Suzetrigine (VX-548) is a small molecule inhibitor and a highly selective inhibitor of the NaV1.8 target, with oral activity and good peripheral nerve selectivity. Suzetrigine is used for the treatment of moderate to severe acute pain following abdominoplasty or bunionectomy.
Targets & IC50
NaV1.8 (dog):740 nM, NaV1.8:0.7 nM, NaV1.8 (mouse):210 nM, NaV1.8 (rabbit):52 nM, NaV1.8 (rat):56 nM, Nav1.8 (human):0.68 ± 0.16 nM, NaV1.8 (monkey):0.75 nM
In vitro
Methods: The inhibitory effect of Suzetrigine was evaluated using automated patch-clamp in HEK, CHO, or ND7/23 cells expressing Nav1.8, and manual patch-clamp in human primary DRG neurons, with incubation at 1–10 nM for 2–10 minutes.
Results: Suzetrigine selectively inhibited Nav1.8 with sub-nanomolar potency (IC50 = 0.68 nM) and concentration-dependently suppressed action potential firing in DRG neurons. [1]
In vivo
Methods: In patients following abdominoplasty or bunionectomy, Suzetrigine was administered at the highest dose (initial oral dose of 100 mg, followed by 50 mg every 12 hours) or a lower dose (initial dose of 20 mg, followed by 10 mg every 12 hours) and compared with placebo to observe changes in acute pain over 48 hours.
Results: Compared with placebo, Suzetrigine reduced acute pain within 48 hours after surgery only at the highest dose.[1]
SynonymsVX-548
Chemical Properties
Molecular Weight473.39
FormulaC21H20F5N3O4
Cas No.2649467-58-1
SmilesC(NC=1C=C(C(N)=O)N=CC1)(=O)[C@H]2[C@@H]([C@H](C)[C@@]([C@@](F)(F)F)(C)O2)C3=C(OC)C(F)=C(F)C=C3
Storage & Solubility Information
StorageStore at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 161 mg/mL (340.1 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1124 mL10.5621 mL21.1242 mL105.6212 mL
5 mM0.4225 mL2.1124 mL4.2248 mL21.1242 mL
10 mM0.2112 mL1.0562 mL2.1124 mL10.5621 mL
20 mM0.1056 mL0.5281 mL1.0562 mL5.2811 mL
50 mM0.0422 mL0.2112 mL0.4225 mL2.1124 mL
100 mM0.0211 mL0.1056 mL0.2112 mL1.0562 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Keywords

Related Tags: Suzetrigine chemical structure | Suzetrigine in vivo | Suzetrigine in vitro | Suzetrigine formula | Suzetrigine molecular weight