| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
VX-150 targets the voltage-gated sodium channel NaV1.8. It acts as a selective inhibitor, blocking sodium influx through this channel. NaV1.8 is primarily expressed in peripheral sensory neurons and plays a key role in pain signaling. By inhibiting NaV1.8, VX-150 reduces the excitability of pain-sensing neurons and provides analgesic effects.
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| ln Vitro |
The prodrug VX-150 is a highly selective NaV1.8 that is converted quickly to the active ingredient and has a restricted channel bioavailability, making it two times more selective than other sodium channel subtypes (>400-fold) [1].
In vitro, VX-150 is a highly selective NaV1.8 inhibitor relative to other sodium channel subtypes (>400-fold). The active moiety of the prodrug potently inhibits NaV1.8-mediated sodium currents. Specific IC50 values are not provided in the available sources. |
| ln Vivo |
In vivo activity data for VX-150 are not extensively detailed in the available sources. The compound is an orally bioavailable prodrug that is being studied for various pain indications. It represents a promising non-opioid analgesic candidate.
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| Enzyme Assay |
The in vitro electrophysiology assay for VX-150 involves measuring the inhibition of NaV1.8 sodium currents. Cells expressing NaV1.8 are patch-clamped, and sodium currents are recorded in the presence of varying compound concentrations. The IC50 is determined by quantifying the reduction in current amplitude.
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| Cell Assay |
Cellular assays for VX-150 are performed using cell lines expressing NaV1.8. Cells are treated with VX-150 or its active metabolite, and sodium influx is measured using fluorescent sodium indicators or by electrophysiological recording. The compound's selectivity for NaV1.8 over other sodium channel subtypes is assessed.
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| Animal Protocol |
In vivo animal studies for VX-150 are conducted in animal models of pain. The compound is administered orally, and its analgesic effects are assessed using behavioral tests such as the formalin test, von Frey filament test, or hot plate test. Specific animal models and dosing regimens are not detailed in the available sources.
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| ADME/Pharmacokinetics |
VX-150 is an orally bioavailable prodrug. It is rapidly converted to its active moiety, which has favorable properties for pain indications. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for VX-150 are not reported in the available sources. As an investigational compound, it is used for research purposes only.
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| References | |
| Additional Infomation |
VX-150 is a research compound being investigated for the treatment of pain. It is a highly selective NaV1.8 inhibitor with a non-opioid mechanism of action. The compound is available from chemical suppliers for research use only.
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| Molecular Formula |
C21H17F4N2O7P
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|---|---|
| Molecular Weight |
516.3363
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| Exact Mass |
516.07
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| CAS # |
1793080-72-4
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| PubChem CID |
118126601
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| Appearance |
White to off-white solid powder
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| Density |
1.59±0.1 g/cm3
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
907
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC(=C1)F)OC2=C(C=CC(=C2)C(F)(F)F)C(=O)NC3=CC(=O)N(C=C3)COP(=O)(O)O
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| InChi Key |
SQDQNNKQTHOQHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17F4N2O7P/c1-12-8-14(22)3-5-17(12)34-18-9-13(21(23,24)25)2-4-16(18)20(29)26-15-6-7-27(19(28)10-15)11-33-35(30,31)32/h2-10H,11H2,1H3,(H,26,29)(H2,30,31,32)
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| Chemical Name |
[4-[[2-(4-fluoro-2-methylphenoxy)-4-(trifluoromethyl)benzoyl]amino]-2-oxopyridin-1-yl]methyl dihydrogen phosphate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~242.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9367 mL | 9.6835 mL | 19.3671 mL | |
| 5 mM | 0.3873 mL | 1.9367 mL | 3.8734 mL | |
| 10 mM | 0.1937 mL | 0.9684 mL | 1.9367 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT06420765
Conditions:PainLink: https://clinicaltrials.gov/ct2/show/NCT05418712
Conditions:PainLink: https://clinicaltrials.gov/ct2/show/NCT03764072
Conditions:Acute Pain
Title:A Study to Evaluate the Efficacy and Safety of VX-150 in Treating Subjects With Pain Caused by Small Fiber Neuropathy
Status:Completed
updateDate:2021-11-15
Ctid:NCT03304522
Link: https://clinicaltrials.gov/ct2/show/NCT03304522
Conditions:Small Fiber NeuropathyLink: https://clinicaltrials.gov/ct2/show/NCT03206749
Conditions:Acute PainLink: https://clinicaltrials.gov/ct2/show/NCT02660424
Conditions:OsteoarthritisProducts are for research use only; We do not sell to patients
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