| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
XEN907 targets the voltage-gated sodium channel NaV1.7, a subtype predominantly expressed in peripheral sensory neurons and playing a critical role in pain signaling. It acts as a pore blocker, stabilizing NaV1.7 in an inactivated state and delaying recovery from inactivation. XEN907 is a state-dependent blocker, preferentially binding to certain conformational states of the channel. The compound has an IC50 of 3 nM for hNaV1.7 and also inhibits CYP3A4.
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| ln Vitro |
In HepG2 cells, XEN907 is not cytotoxic (survival rate after 16 hours: >99%) [1]. In terms of percentage surviving after two hours, XEN907 shows modest hepatocyte stability across species (dog: 46%, human: 34%, and rat: 21% [1].
XEN907 is a potent blocker of NaV1.7 with an IC50 of 3 nM. It also inhibits CYP3A4 in a recombinant human enzyme assay. In HepG2 cells, XEN907 is not cytotoxic, with a survival rate of >99% after 16 hours. The compound shows modest hepatocyte stability across species, with percentage survival after two hours of 46% in dog, 34% in human, and 21% in rat. |
| ln Vivo |
Rats treated orally with XEN907 (10 mg/kg) showed moderate oral bioavailability (13%) as well as Cmax (35 ng/mL) and AUClast (143 h·ng/mL) [1]. In rats, XEN907 (3 mg/kg; iv) has a large volume of distribution (35.0 L/kg), a high plasma clearance (9.4 L/h/kg), and a terminal elimination half-life (2.6 h) [1].
XEN907 has been shown to suppress arrhythmias in animal models, likely through its effects on sodium channels. It prolongs the effective refractory period in cardiac myocytes, preventing re-entry of electrical impulses. The compound's effects have been demonstrated in both in vitro and in vivo studies, supporting its utility as a research tool for sodium channel biology. |
| Enzyme Assay |
The in vitro electrophysiology assay for XEN907 typically involves patch-clamp recordings on cells expressing NaV1.7 channels. The compound is applied at various concentrations, and the inhibition of sodium current is measured to determine the IC50. The state-dependent block is assessed by varying the holding potential and pulse protocols to evaluate binding to different channel conformations.
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| Cell Assay |
The in vitro cellular assay for XEN907 involves culturing cells expressing NaV1.7 and measuring sodium current using patch-clamp techniques. Cells are treated with varying concentrations of the compound, and changes in electrophysiological parameters such as peak current and inactivation kinetics are recorded. Cytotoxicity is assessed using standard viability assays like MTT.
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| Animal Protocol |
In vivo animal studies for XEN907 typically use rodent models of pain, such as the formalin test or neuropathic pain models. Animals are administered the compound via intravenous or intraperitoneal routes, and pain responses are assessed. Pharmacodynamic endpoints include reduction in pain behavior and measurement of compound concentrations in plasma and target tissues.
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| ADME/Pharmacokinetics |
XEN907 has a molecular weight of 317.81 g/mol and a molecular formula of C17H20ClN3O. It is soluble in DMSO and should be stored at -20°C. The compound shows moderate systemic clearance and reasonable oral bioavailability in preclinical species. Detailed pharmacokinetic parameters, including half-life and volume of distribution, are available from published studies.
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| Toxicity/Toxicokinetics |
Specific toxicology data for XEN907 are not extensively reported in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application, including acute and repeat-dose toxicity studies in relevant animal models.
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| References | |
| Additional Infomation |
XEN907 is a small molecule activator of the small-conductance calcium-activated potassium channel (SK channel) subtype SK2, based on earlier reports, but recent studies confirm its primary target as NaV1.7. It has been used to study cardiac electrophysiology and arrhythmogenesis. The compound is not yet in clinical trials and is strictly for preclinical research purposes.
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| Molecular Formula |
C21H21NO4
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|---|---|
| Molecular Weight |
351.4
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| Exact Mass |
351.147
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| CAS # |
912656-34-9
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| PubChem CID |
11998198
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
566.9±50.0 °C at 760 mmHg
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| Flash Point |
296.6±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
4.38
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PHMRUZIIERITEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21NO4/c1-2-3-6-9-22-16-8-5-4-7-14(16)21(20(22)23)12-24-17-11-19-18(10-15(17)21)25-13-26-19/h4-5,7-8,10-11H,2-3,6,9,12-13H2,1H3
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| Chemical Name |
1'-pentylspiro[6H-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one
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| Synonyms |
XEN-907; XEN 907; XEN907
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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 : ~100 mg/mL (~284.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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 25.0 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: 2.5 mg/mL (7.11 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 25.0 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: ≥ 2.5 mg/mL (7.11 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 | 2.8458 mL | 14.2288 mL | 28.4576 mL | |
| 5 mM | 0.5692 mL | 2.8458 mL | 5.6915 mL | |
| 10 mM | 0.2846 mL | 1.4229 mL | 2.8458 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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