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Synonyms: VX-548


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $53 | In Stock | In Stock | |
| 5 mg | $116 | In Stock | In Stock | |
| 10 mg | $173 | In Stock | In Stock | |
| 25 mg | $281 | In Stock | In Stock | |
| 50 mg | $482 | In Stock | In Stock | |
| 100 mg | $786 | In Stock | In Stock | |
| 200 mg | $1,080 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $120 | In Stock | In Stock |
| 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] |
| Synonyms | VX-548 |
| Molecular Weight | 473.39 |
| Formula | C21H20F5N3O4 |
| Cas No. | 2649467-58-1 |
| Smiles | C(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 | Store 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
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. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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