| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
TC-AQP1-1 targets aquaporin 1 (AQP1), a water channel protein that facilitates rapid water transport across cell membranes. AQP1 is involved in various physiological processes including renal water reabsorption, cerebrospinal fluid production, and cell migration. By blocking the AQP1 channel, TC-AQP1-1 inhibits water flux through the channel, making it a valuable tool for studying AQP1 function.
|
|---|---|
| ln Vitro |
In vitro, TC-AQP1-1 inhibits AQP1-mediated water flux in Xenopus laevis oocytes with an IC50 of 8 μM. The compound acts as a potent AQP1 inhibitor. Its activity is assessed by measuring the inhibition of water transport through AQP1 channels expressed in oocytes or other heterologous expression systems.
|
| ln Vivo |
In vivo, TC-AQP1-1 has been used to study the role of AQP1 in various physiological and pathological processes. By inhibiting AQP1-mediated water transport, the compound can affect fluid homeostasis, cell migration, and angiogenesis. It is used as a research tool to investigate the function of AQP1 in health and disease.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for TC-AQP1-1 measure its inhibition of AQP1-mediated water transport. Oocytes expressing human AQP1 are incubated with the compound, and water flux is measured by assessing oocyte swelling in hypotonic solutions. The IC50 of 8 μM is determined from dose-response curves. The compound's selectivity for AQP1 over other aquaporins can be assessed using similar assays.
|
| Cell Assay |
In vitro cell-based assays for TC-AQP1-1 use cells expressing AQP1, such as Xenopus laevis oocytes or mammalian cell lines. Cells are treated with serial dilutions of the compound, and water permeability is measured by monitoring cell volume changes in response to osmotic gradients. The IC50 for inhibition of AQP1-mediated water flux is calculated from dose-response curves.
|
| Animal Protocol |
In vivo animal models for TC-AQP1-1 include models of conditions involving AQP1, such as cerebral edema, renal disease, or angiogenesis. The compound is administered systemically or locally, and its effects on fluid balance, tissue water content, and disease progression are evaluated. Pharmacodynamic studies measure AQP1 inhibition in target tissues.
|
| ADME/Pharmacokinetics |
TC-AQP1-1 has a molecular formula of C12H10O4 and a molecular weight of 218.21 g/mol. It is soluble in DMSO at approximately 50 mg/mL (229.14 mM). For in vivo administration, it can be formulated in 10% DMSO + 90% Corn Oil at ≥2.5 mg/mL. The compound is stored as a powder at -20°C for up to 3 years.
|
| Toxicity/Toxicokinetics |
The toxicity profile of TC-AQP1-1 is characterized in preclinical studies. As an AQP1 inhibitor, the compound may affect water homeostasis in tissues expressing AQP1. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
|
| References | |
| Additional Infomation |
TC-AQP1-1 is also known as m-Phenylenediacrylic acid or m-Benzenediacrylic acid. It is a potent AQP1 inhibitor that inhibits AQP1-mediated water flux in oocytes with an IC50 of 8 μM. The compound was identified by virtual screening. It is intended for laboratory research use only and is not for human use.
|
| Molecular Formula |
C12H10O4
|
|---|---|
| Molecular Weight |
218.208
|
| Exact Mass |
218.058
|
| Elemental Analysis |
C, 66.05; H, 4.62; O, 29.33
|
| CAS # |
37710-81-9
|
| PubChem CID |
794091
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.882
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
16
|
| Complexity |
287
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(/C=C/C(O)=O)C=CC=C(/C=C/C(O)=O)C=1
|
| InChi Key |
KRXUBZPHAPGHPE-YDFGWWAZSA-N
|
| InChi Code |
InChI=1S/C12H10O4/c13-11(14)6-4-9-2-1-3-10(8-9)5-7-12(15)16/h1-8H,(H,13,14)(H,15,16)/b6-4+,7-5+
|
| Chemical Name |
(E)-3-[3-[(E)-2-carboxyethenyl]phenyl]prop-2-enoic acid
|
| Synonyms |
TC-AQP1-1TC-AQP 1-1TC-AQP-1-1
|
| 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) |
DMSO : ~50 mg/mL (~229.14 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5827 mL | 22.9137 mL | 45.8274 mL | |
| 5 mM | 0.9165 mL | 4.5827 mL | 9.1655 mL | |
| 10 mM | 0.4583 mL | 2.2914 mL | 4.5827 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.