Suzetrigine

Boiling point: 591.8±50.0°C

Density: 1.399±0.06 g/cm3

Storage temp: Hygroscopic, -20°C Freezer, Under inert atmosphere

Solubility:Acetonitrile: Slightly Soluble: 0.1-1 mg/mL DMSO: Sparingly Soluble: 1-10 mg/mL

Form: Solid

Color: White to Light Yellow

Cell Experiment

DMSO : 116.67 mg/mL (246.46 mM; Need ultrasonic)

Preparing Stock Solutions：

Please select an appropriate solvent to prepare the stock solution according to the product's solubility in different solvents. Once dissolved, aliquot the solution and store it to avoid product failure caused by repeated freeze-thaw cycles. Storage conditions and shelf life: -80°C for 6 months; -20°C for 1 month. When stored at -80°C, please use within 6 months; when stored at -20°C, please use within 1 month.

Suzetrigine works to attenuate pain signals. In a clinical trial involving patients with acute pain following abdominoplasty and bunionectomy, treatment with suzetrigine was associated with significantly decreased pain scores compared with placebo.

It displays a selective binding profile. In human dorsal root ganglion neurons, suzetrigine exhibited over 31000-times greater selectivity for NaV1.8 than other NaV subtypes. Its potency was high with IC50 (50% of maximal inhibitory concentration) of 0.68 ± 0.16 nM.

Suzetrigine is a selective blocker of the NaV1.8 voltage-gated sodium channel, which is expressed in peripheral nociceptive neurons, including dorsal root ganglion neurons, to play a role in transmitting nociceptive signals.By blocking the sodium channels, suzetrigine stops the transmission of pain signals to the spinal cord and brain. M6-SUZ, the primary active metabolite, is 3.7 times less potent than suzetrigine as an inhibitor of NaV1.8.