Cat. No.: HY-148800

Suzetrigine

(Synonyms: VX-548)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Suzetrigine (VX-548) is an orally active and highly selective Na_V1.8 inhibitor that acts as an analgesic. Suzetrigine is also a blocker of sodium channel protein type 10 subunit alpha. Suzetrigine is promising for research of acute pain after abdominoplasty and bunionectomy.

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

Purity: 99.98%
CAS No.: 2649467-58-1
Formula: C₂₁H₂₀F₅N₃O₄
Molecular Weight:473.39

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Suzetrigine Chemical Structure

CAS No.: 2649467-58-1

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Top Publications Citing

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Sodium Channel Isoforms :

In Vivo

Pharmacokinetic parameters of Suzetrigine in monkey plasma after oral and intravenous administrations^[3]

Parameters	AUC_0-t (ng·h/mL)	C_max (ng/mL)	T_max (h)	T_1/2 (h)	CL (mL/min/kg)	V_d (L/kg)	MRT_0-t (h)	F (%)
Intravenous (1 mg/kg, n = 3)	2843.2 ± 350.2	-	-	4.6 ± 0.2	5.8 ± 0.6	2.3 ± 0.4	5.7 ± 0.2	71
Oral (2 mg/kg, n = 3)	4040.8 ± 212.5	533.3 ± 10.6	1	5.0 ± 0.9	7.2 ± 0.5	3.5 ± 0.6	7.6 ± 0.7

Pharmacokinetic parameters of Suzetrigine rats after intravenous administration at a single dose of 1 mg/kg^[4]

Parameters	AUC_0-t (ng·h/mL)	T_1/2 (h)	CL (mL/min/kg)	V_ss (L/kg)	MRT_0-t (h)
Female (n = 3)	1505.8 ± 47.3	3.7 ± 0.4	12.5 ± 0.8	5.0 ± 1.0	6.4 ± 0.3
Male (n = 3)	253.8 ± 6.3	1.9 ± 0.2	65.1 ± 1.7	7.2 ± 0.8	1.7 ± 0.2

Pharmacokinetic parameters of Suzetrigine rats after oral administration at a single dose of 2 mg/kg^[4]

Parameters	AUC_0-t (ng·h/mL)	T_1/2 (h)	C_max (ng/mL)	T_max (h)	F (%)
Female (n = 3)	2905.2 ± 98.6	4.9 ± 0.5	369.6 ± 62.2	0.5-1	96
Male (n = 3)	56.9 ± 18.5	2.5 ±0.2	31.7 ± 12.5	0.5-1	11

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2649467-58-1
Appearance Solid
Molecular Weight 473.39
Formula C₂₁H₂₀F₅N₃O₄
Color White to light yellow
SMILES

NC(C1=CC(NC([C@H]2[C@H](C3=C(C(F)=C(C=C3)F)OC)[C@@H]([C@@](C)(O2)C(F)(F)F)C)=O)=CC=N1)=O
Synonyms

VX-548
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

Publications (6)

All Bio/Physico-chemical Assay

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Journal Impact Factor

FASEB J

The Excelsatoxin A-Receptor TMEM233 Modulates Nav1.8. [Abstract]

2026 Mar 31;40(6):e71706. PMID: 41854608
Mol Pharmacol

Identification and characterization of selective inhibitors of Nav1.9 voltage dependent sodium channels. [Abstract]

2026 May-Jun;108(5-6):100125. PMID: 42167068
J Gen Physiol

Differential state-dependent Nav1.8 inhibition by suzetrigine, LTGO-33, and A-887826. [Abstract]

2025 Jul 7;157(4):e202413719. PMID: 40136042

Suzetrigine purchased from MedChemExpress. Usage Cited in: J Gen Physiol. 2025 Jul 7;157(4):e202413719. [Abstract]

Test for reverse use dependence using an AP waveform recorded from a human DRG neuron at 37°C, delivered at 20 Hz. Same for application of 1 nM VX-548.

Suzetrigine purchased from MedChemExpress. Usage Cited in: J Gen Physiol. 2025 Jul 7;157(4):e202413719. [Abstract]

Same for 1 nM VX-548 (red, n = 7). Solid line: Boltzmann function with midpoint +33 mV, slope factor 16.3 mV.
Biopharm Drug Dispos

Gender difference in the pharmacokinetics and metabolism of VX-548 in rats. [Abstract]

2024 Apr;45(2):107-114. PMID: 38573807
bioRxiv

2026 Mar 3.
bioRxiv

2025 April 15.

Suzetrigine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 April 15.

Representative raw trace example showing an MDA patient DRG neuron with ectopic discharge at baseline that ceased action potential (AP) firing and became hyperpolarized after application of Suzetrigine (10 nM; 1 min), as indicated by the blue bar above the trace.

Suzetrigine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 April 15.

Suzetrigine (10 nM; 10 ms). where the pre-drug AP waveform is shown in black and the post-drug AP waveform is shown in blue.

Suzetrigine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 April 15.

Evoked excitability was produced by a ramp stimulus applying a 1-100 pA ramp over 1 s, increasing the ramp end point by 200 pA each sweep. During VX-548 (10 nM) perfusion, the number of action potentials fired in each sweep significantly reduced relative to bath perfusion alone in the same cell.

Solvent & Solubility

In Vitro:

DMSO : 116.67 mg/mL (246.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1124 mL

10.5621 mL

21.1242 mL

5 mM

0.4225 mL

2.1124 mL

4.2248 mL

10 mM

0.2112 mL

1.0562 mL

2.1124 mL

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

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jones J, et al. Selective Inhibition of NaV1.8 with VX-548 for Acute Pain. N Engl J Med. 2023 Aug 3;389(5):393-405. [Content Brief]

[2]. WHO Drug Information-World Health Organization (WHO).

[3]. Zhang H, et al. A simple and sensitive ultra-high performance liquid chromatography tandem mass spectrometry method for the quantitative analysis of VX-548 in monkey plasma: Method validation and application to pharmacokinetic study. Biomed Chromatogr. 2024 Jul;38(7):e5907. [Content Brief]

[4]. Yu G, et al. Gender difference in the pharmacokinetics and metabolism of VX-548 in rats. Biopharm Drug Dispos. 2024 Apr;45(2):107-114. [Content Brief]

[5]. Qin H, et al. Discovery of selective NaV1.8 inhibitors based on 5-chloro-2-(4,4-difluoroazepan-1-yl)-6-methyl nicotinamide scaffold for the treatment of pain. Eur J Med Chem. 2023 Jun 5;254:115371. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.1124 mL	10.5621 mL	21.1242 mL	52.8106 mL
	5 mM	0.4225 mL	2.1124 mL	4.2248 mL	10.5621 mL
	10 mM	0.2112 mL	1.0562 mL	2.1124 mL	5.2811 mL
	15 mM	0.1408 mL	0.7041 mL	1.4083 mL	3.5207 mL
	20 mM	0.1056 mL	0.5281 mL	1.0562 mL	2.6405 mL
	25 mM	0.0845 mL	0.4225 mL	0.8450 mL	2.1124 mL
	30 mM	0.0704 mL	0.3521 mL	0.7041 mL	1.7604 mL
	40 mM	0.0528 mL	0.2641 mL	0.5281 mL	1.3203 mL
	50 mM	0.0422 mL	0.2112 mL	0.4225 mL	1.0562 mL
	60 mM	0.0352 mL	0.1760 mL	0.3521 mL	0.8802 mL
	80 mM	0.0264 mL	0.1320 mL	0.2641 mL	0.6601 mL
	100 mM	0.0211 mL	0.1056 mL	0.2112 mL	0.5281 mL

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Suzetrigine

Membrane Transporter/Ion Channel Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Suzetrigine

All Sodium Channel Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Suzetrigine

Membrane Transporter/Ion Channel Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Suzetrigine

All Sodium Channel Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Suzetrigine Related Classifications

HY-148800 Related Classifications