| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
RN1747 targets the transient receptor potential cation channel TRPV4 (TRPV4). As a selective agonist, it activates TRPV4 channels, leading to calcium influx and downstream signaling. It also antagonizes TRPM8 channels with an IC50 of 4 µM. Its dual activity on TRP channels makes it a valuable tool for studying TRP channel biology. Its EC50 values vary across species.
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| ln Vitro |
In vitro, RN1747 acts as a selective TRPV4 agonist with EC50 values of 0.77 µM for human TRPV4, 4.0 µM for mouse TRPV4, and 4.1 µM for rat TRPV4. It also antagonizes TRPM8 with an IC50 of 4 µM. Its activity is confirmed in calcium flux assays using cells expressing TRPV4 or TRPM8 channels. It shows selectivity over other TRP channels.
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| ln Vivo |
In vivo, RN1747 has been used to study TRPV4-mediated physiological processes such as osmosensation, thermoregulation, and mechanotransduction. However, specific in vivo efficacy data in animal models are limited. Its dual activity on TRPV4 and TRPM8 makes it a useful tool for studying TRP channel function in vivo.
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| Enzyme Assay |
Cell-free assays for RN1747 are not standard because it targets ion channels. Its activity is assessed using calcium flux assays or electrophysiological techniques on cells expressing TRPV4 or TRPM8 channels. The EC50 for TRPV4 activation and IC50 for TRPM8 antagonism are determined. Its purity is confirmed by HPLC.
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| Cell Assay |
Cellular assays for RN1747 are performed using cell lines expressing TRPV4 or TRPM8 channels. Cells are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of RN1747. Calcium influx is measured using a fluorometric plate reader. The EC50 for TRPV4 activation and IC50 for TRPM8 inhibition are determined.
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| Animal Protocol |
In vivo animal experiments for RN1747 are not extensively documented. To study TRPV4 function, animal models of pain, inflammation, or osmoregulation could be used. Animals would be administered RN1747 via appropriate routes, and physiological or behavioral endpoints would be assessed.
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| ADME/Pharmacokinetics |
RN1747 has a molecular weight of 404.26 g/mol and a molecular formula of C19H17Cl2N3O3. It has a purity of >97%. It is soluble in DMSO and should be stored under recommended conditions. Its chemical name is not specified in the available sources.
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| Toxicity/Toxicokinetics |
The toxicological profile of RN1747 has not been extensively characterized. As a research compound, it is generally considered safe at the concentrations used in studies. No significant toxicity has been reported. It is not an approved drug and is intended for research use only.
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| References | |
| Additional Infomation |
RN1747 is a selective TRPV4 agonist and TRPM8 antagonist. It has EC50 values of 0.77 µM (human), 4.0 µM (mouse), and 4.1 µM (rat) for TRPV4, and an IC50 of 4 µM for TRPM8. It is widely used in studies exploring calcium signaling, osmosensation, thermoregulation, and mechanotransduction. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C17H18CLN3O4S
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|---|---|
| Molecular Weight |
395.86
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| Exact Mass |
395.071
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| CAS # |
1024448-59-6
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| Related CAS # |
1024448-59-6;
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| PubChem CID |
5068295
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.234
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
578
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZNLVYSJQUMALEO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18ClN3O4S/c18-15-6-7-17(16(12-15)21(22)23)26(24,25)20-10-8-19(9-11-20)13-14-4-2-1-3-5-14/h1-7,12H,8-11,13H2
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| Chemical Name |
1-benzyl-4-[(4-chloro-2-nitrobenzene)sulfonyl]piperazine
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| Synonyms |
RN1747 RN 1747 RN-1747.
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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 : ~50 mg/mL (~126.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.25 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 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.25 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 20.8 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: ≥ 2.08 mg/mL (5.25 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 | 2.5261 mL | 12.6307 mL | 25.2615 mL | |
| 5 mM | 0.5052 mL | 2.5261 mL | 5.0523 mL | |
| 10 mM | 0.2526 mL | 1.2631 mL | 2.5261 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.