| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Nav1.7 <3.2 nM (IC50)
The primary target of GX-201 is the voltage-gated sodium channel Nav1.7, which is predominantly expressed in peripheral sensory neurons and plays a critical role in pain signaling. GX-201 is a potent and selective Nav1.7 blocker with an IC50 of <3.2 nM for hNaV1.7. By inhibiting Nav1.7, GX-201 blocks the initiation and propagation of action potentials in pain-sensing neurons, thereby exerting analgesic effects. The compound's high potency and selectivity make it a valuable tool for pain research and a potential therapeutic candidate. |
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| ln Vitro |
In vitro, GX-201 is a potent inhibitor of Nav1.7 with an IC50 of <3.2 nM for hNaV1.7. The compound's high selectivity for Nav1.7 over other sodium channels is a key feature that contributes to its analgesic potential. GX-201 is a small molecule that can be used to study the role of Nav1.7 in pain signaling. It is available with a purity of >99% and has a molecular weight of 563 g/mol.
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| ln Vivo |
In mice, GX -201 has a comparatively lengthy half-life[1]. Analgesia is produced by GX-201 at a free plasma concentration that is around three times the IC50[1]. Complete Freund's adjuvant (CFA)-induced inflammatory pain is inhibited by GX-201, as is the nociceptive response caused by formalin[1].
In vivo, GX-201 produces analgesic effects in animal models of pain. It suppresses formalin-induced nociceptive responses and inflammatory pain caused by complete Freund's adjuvant (CFA). The compound has a relatively long half-life in mice, and analgesic effects are observed at free plasma concentrations approximately three times the IC50 for high-affinity channel blockade. GX-201 is a potent and selective Nav1.7 blocker and an analgesic. |
| Enzyme Assay |
In vitro assays for GX-201 typically involve measuring its inhibition of Nav1.7 channel activity using electrophysiological techniques such as patch-clamp recording in cell lines expressing recombinant hNaV1.7 channels. The compound is applied to the cells at varying concentrations (typically 0.1-100 nM), and the resulting inhibition of sodium current is measured. The IC50 of <3.2 nM is determined by fitting concentration-response curves. Selectivity assays against other sodium channel subtypes (NaV1.1-1.8) are also performed to assess the compound's specificity.
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| Cell Assay |
Cellular assays for GX-201 typically use cell lines expressing recombinant Nav1.7 channels, such as HEK293 or CHO cells. The compound is applied to the cells, and its effects on channel activity are assessed using electrophysiological techniques such as patch-clamp recording. Fluorescent-based membrane potential assays using voltage-sensitive dyes can also be used for higher-throughput screening of channel activity. Cells are treated with GX-201 at various concentrations (e.g., 0.1-100 nM), and the inhibition of sodium current or changes in membrane potential are measured. The IC50 for channel inhibition is determined from the concentration-response data.
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| Animal Protocol |
Animal/Disease Models: Wild-Type Mice[1].
Doses: 0.3, 1, 3 mg/kg. Route of Administration: Orally, once. Experimental Results: Produced a dose-dependent inhibition of the nociceptive events. In vivo animal studies for GX-201 have been conducted in rodent models of pain. The compound is typically administered via intraperitoneal injection or oral gavage. In the formalin test, GX-201 suppresses nociceptive responses, demonstrating its analgesic effects in acute pain models. In the complete Freund's adjuvant (CFA)-induced inflammatory pain model, GX-201 reduces pain-related behaviors. Pharmacokinetic parameters, such as plasma half-life, are also assessed in these studies. GX-201 has a relatively long half-life in mice. |
| ADME/Pharmacokinetics |
GX-201 has a relatively long half-life in mice. The compound has a molecular weight of 563 g/mol and a molecular formula of C25H27ClF4N2O4S. It is available with a purity of >99%. For research purposes, the compound is typically stored under recommended conditions as per the Certificate of Analysis. Detailed parameters such as volume of distribution and bioavailability are not fully available in the public domain but are characteristic of small molecule Nav1.7 inhibitors.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for GX-201 in the available literature. As a research chemical intended for laboratory use only, it should be handled with standard safety precautions for handling chemical reagents. The compound is not approved for human therapeutic use. Researchers should consult the material safety data sheet (MSDS) for detailed safety and handling information. Any potential toxicity would need to be assessed through formal toxicological studies if the compound were to be developed further.
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| References | |
| Additional Infomation |
GX-201 is a potent and selective Nav1.7 inhibitor with an IC50 of <3.2 nM for hNaV1.7. It has a molecular formula of C25H27ClF4N2O4S and a molecular weight of 563 g/mol. GX-201 produces analgesic effects in vivo, suppresses formalin-induced nociceptive responses, and reduces CFA-induced inflammatory pain. It has a relatively long half-life in mice and is an analgesic compound. GX-201 is available with a purity of >99%.
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| Molecular Formula |
C25H27CLF4N2O4S
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|---|---|
| Molecular Weight |
563.004498720169
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| Exact Mass |
562.131
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| CAS # |
1788071-27-1
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| PubChem CID |
118120545
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
890
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=C(C(F)(F)F)C=C1CN1CCC(COC2=CC(=C(C(NS(C)(=O)=O)=O)C=C2C2CC2)F)CC1
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| InChi Key |
KYBPOTYVFWNSGS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27ClF4N2O4S/c1-37(34,35)31-24(33)20-11-19(16-2-3-16)23(12-22(20)27)36-14-15-6-8-32(9-7-15)13-17-10-18(25(28,29)30)4-5-21(17)26/h4-5,10-12,15-16H,2-3,6-9,13-14H2,1H3,(H,31,33)
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| Chemical Name |
4-[[1-[[2-chloro-5-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide
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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: 62.5 mg/mL (111.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7762 mL | 8.8810 mL | 17.7620 mL | |
| 5 mM | 0.3552 mL | 1.7762 mL | 3.5524 mL | |
| 10 mM | 0.1776 mL | 0.8881 mL | 1.7762 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.
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