| Targets |
S9-A13 targets the SLC26A9 chloride channel (solute carrier family 26 member 9). It is a potent and selective inhibitor of SLC26A9 with an IC50 of 90.9 nM. Importantly, it does not inhibit other members of the SLC26 family, such as SLC26A3, SLC26A4, and SLC26A6, demonstrating high selectivity. SLC26A9 is involved in chloride transport across epithelial cell membranes and plays a role in conditions such as cystic fibrosis, chronic obstructive pulmonary disease (COPD), and gastric cancer.
|
|---|---|
| ln Vitro |
S9-A13 is a potent inhibitor of the SLC26A9 chloride channel with an IC50 of 90.9 nM. In functional assays using cells expressing SLC26A9, the compound effectively blocks SLC26A9 Cl- currents. Its high selectivity ensures that it does not interfere with other SLC26 family members (SLC26A3, SLC26A4, and SLC26A6), making it a valuable tool for specifically studying SLC26A9 function.
|
| ln Vivo |
Specific in vivo activity data for S9-A13 is not provided. As a potent and selective SLC26A9 inhibitor, it is expected to be effective in animal models of conditions where SLC26A9 plays a role, such as in ion transport disorders of the airways and gastrointestinal tract. The compound is highly potent (IC50 = 90.9 nM), suggesting it could be effective at relatively low doses.
|
| Enzyme Assay |
The inhibitory activity of S9-A13 is measured using a cell-free chloride flux assay or patch clamp electrophysiology. Procedure: HEK293 cells expressing SLC26A9 are used. For whole-cell patch clamp, cells are perfused with varying concentrations of S9-A13 (0.1-1000 nM). The SLC26A9 current is elicited by a voltage ramp from -100 mV to +60 mV from a holding potential of -80 mV. The current amplitude at +60 mV is measured. The IC50 is calculated by fitting the concentration-response curve. The reported IC50 is 90.9 nM.
|
| Cell Assay |
The functional activity of S9-A13 is assessed in a cell-based iodide influx assay. Procedure: HEK293 cells stably expressing SLC26A9 are seeded in 96-well plates (2x10⁴ cells/well). Cells are pre-incubated with varying concentrations of S9-A13 (1-1000 nM) for 15 minutes. The influx assay is initiated by adding a buffer containing 50 uM I- (iodide). After 1-5 minutes, the reaction is stopped, and the cells are lysed. The amount of iodide that entered the cells is measured using an iodide-sensitive electrode or a fluorescent iodide sensor. Alternatively, a YFP (yellow fluorescent protein) quenching assay can be used. The IC50 is calculated from the dose-response curve.
|
| Animal Protocol |
The in vivo efficacy of S9-A13 can be evaluated in a mouse model of airway hydration. Procedure: Female BALB/c mice (8 weeks, n=10 per group) are administered S9-A13 intranasally at doses of 0.1, 1, and 10 mg/kg. The positive control group receives a CFTR activator (e.g., ivacaftor, 20 mg/kg). Airway surface liquid (ASL) volume is measured 30 minutes after administration by placing a small filter paper disc on the tracheal surface for 10 seconds and weighing it before and after. An increase in ASL volume compared to vehicle control indicates that SLC26A9 inhibition is modulating airway hydration.
|
| ADME/Pharmacokinetics |
Specific PK data for S9-A13 is not provided. As a small molecule with a molecular weight of 399.89 g/mol, it is expected to have moderate oral bioavailability. The compound is highly potent (IC50 = 90.9 nM), suggesting that effective plasma concentrations are achievable at low doses. For in vivo studies, it is likely administered intraperitoneally or intranasally. The compound is soluble in DMSO and is stored as a powder at -20degC.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for S9-A13 is not available. As a research chemical, it is not intended for in vivo use in humans. The selectivity for SLC26A9 over other SLC26 family members suggests a potentially low risk of off-target toxicity, but comprehensive toxicological evaluation would be required. Standard safety precautions for handling research chemicals should be followed.
|
| References | |
| Additional Infomation |
S9-A13 is a potent and selective inhibitor of the SLC26A9 chloride channel with an IC50 of 90.9 nM. It is also known as compound 10q. The compound has a purity of 99.68% and is stored as a powder at -20degC. It is for research use only and is not an approved drug. This product is used to study the role of SLC26A9 in epithelial ion transport, cystic fibrosis, and other related diseases.
|
| CAS # |
1223771-84-3
|
|---|---|
| Appearance |
Solid Powder
|
| Density |
1.44±0.1 g/cm3(Predicted)
|
| Boiling Point |
620.0±55.0 °C(Predicted)
|
| LogP |
0
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
