| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 250mg | |||
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| Targets |
Epithelial chloride channels; the R(+)-IAA-94 exhibited inhibitory activity against epithelial chloride channels, with an IC50 value of approximately 10 μM in experiments using canine tracheal epithelial cells [1]
Epithelial chloride channels purified from kidney and trachea; R(+)-IAA-94 inhibited the activity of these reconstituted chloride channels [2] |
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| ln Vitro |
Chloride channel function has been modulated by IAA-94 in order to examine channel dynamics and function. These proteins have been isolated and reconstituted thanks to IAA-94's strong affinity for chloride channels [1][2].
In canine tracheal epithelial cells cultured in vitro, R(+)-IAA-94 dose-dependently inhibited chloride ion transport across the cell membrane. At a concentration of 30 μM, the inhibitory rate of chloride transport reached over 80% compared to the control group [1] When purified epithelial chloride channels from kidney and trachea were reconstituted into artificial lipid bilayers, R(+)-IAA-94 (at 15 μM) reduced the open probability of the chloride channels by approximately 60%, and the inhibitory effect was reversible upon washout of the drug [2] |
| Enzyme Assay |
For the detection of epithelial chloride channel activity (target binding assay), membrane vesicles containing epithelial chloride channels were prepared from canine tracheal epithelial cells. The vesicles were incubated with different concentrations of R(+)-IAA-94 (0.1–100 μM) for 30 minutes at 37°C. Then, the chloride ion flux through the channels was measured using a chloride-selective electrode, and the changes in chloride flux were used to calculate the inhibitory activity of the drug on the channels [1]
For the reconstituted chloride channel activity assay, purified chloride channels from kidney and trachea were mixed with lipid solutions to form liposomes. The liposomes were exposed to R(+)-IAA-94 (1–50 μM) for 20 minutes, and then the channel current was recorded using the patch-clamp technique in the whole-cell configuration. The current amplitude and open time of the channels were analyzed to evaluate the inhibitory effect of the drug [2] |
| Cell Assay |
Canine tracheal epithelial cells were seeded in 6-well plates and cultured until confluent. The culture medium was replaced with a buffer containing R(+)-IAA-94 at concentrations of 1 μM, 10 μM, 30 μM, and 100 μM, with a drug-free buffer as the control. After incubating for 2 hours at 37°C, the cells were harvested, and the intracellular chloride ion concentration was measured using a fluorescent chloride probe. The results were used to assess the effect of R(+)-IAA-94 on chloride ion homeostasis in epithelial cells [1]
Epithelial cells isolated from rat kidney were cultured on permeable supports to form polarized monolayers. R(+)-IAA-94 was added to either the apical or basolateral side of the monolayers at a concentration of 20 μM. The transepithelial chloride current was measured using an Ussing chamber system every 15 minutes for 2 hours to determine the side-specific inhibitory effect of the drug on chloride transport [2] |
| References |
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| Additional Infomation |
R(+)-IAA-94 is a synthetic ligand specifically developed for studying the function of epithelial chloride channels. Its inhibitory effect is stereoselective—the S(-)-enantiomer of IAA-94 has significantly weaker inhibitory activity on epithelial chloride channels than the R(+)-enantiomer[1]. The inhibitory effect of R(+)-IAA-94 on reconstituted chloride channels in the kidney and trachea indicates that the drug acts directly on chloride channel proteins rather than through indirect cell signaling pathways[2].
|
| Molecular Formula |
C17H18O4CL2
|
|---|---|
| Molecular Weight |
357.22842
|
| Exact Mass |
356.058
|
| CAS # |
54197-31-8
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| Related CAS # |
(Rac)-Methylindazone;53108-00-2
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| PubChem CID |
3667
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| Appearance |
White to yellow solid powder
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| Density |
1.401g/cm3
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| Boiling Point |
537.2ºC at 760 mmHg
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| Flash Point |
278.7ºC
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| Index of Refraction |
1.597
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| LogP |
4.392
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
491
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RNOJGTHBMJBOSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18Cl2O4/c1-17(10-4-2-3-5-10)7-9-6-11(23-8-12(20)21)14(18)15(19)13(9)16(17)22/h6,10H,2-5,7-8H2,1H3,(H,20,21)
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| Chemical Name |
2-[(6,7-dichloro-2-cyclopentyl-2-methyl-1-oxo-3H-inden-5-yl)oxy]acetic acid
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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 (~279.93 mM)
H2O : ~0.1 mg/mL (~0.28 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.00 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 (7.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (7.00 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 | 2.7993 mL | 13.9966 mL | 27.9932 mL | |
| 5 mM | 0.5599 mL | 2.7993 mL | 5.5986 mL | |
| 10 mM | 0.2799 mL | 1.3997 mL | 2.7993 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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