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RN1747

Alias: RN1747 RN 1747 RN-1747.
Cat No.:V13838 Purity: ≥98%
RN1747 is a selective TRPV4 agonist (EC50 are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively).
RN1747
RN1747 Chemical Structure CAS No.: 1024448-59-6
Product category: TRP Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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25mg
50mg
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250mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
RN1747 is a selective TRPV4 agonist (EC50 are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively). RN1747 exhibits selectivity over other TRP channels (EC50 are 0.77, >30, >30 and >100 μM for TRPV4, TRPM8, TRPV3 and TRPV1 receptors respectively). It also antagonizes TRPM8 at relevant concentrations (IC50 = 4 μM).
RN1747 (CAS#: 1024448-59-6) is a selective TRPV4 channel agonist with EC50 values of 0.77 µM (human), 4.0 µM (mouse), and 4.1 µM (rat). It also acts as a TRPM8 antagonist with an IC50 of 4 µM. RN1747 is widely used in studies exploring calcium signaling, osmosensation, thermoregulation, and mechanotransduction.
Biological Activity I Assay Protocols (From Reference)
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.
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.
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.
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.
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.
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.
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.
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.
References

[1]. Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4.

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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H18CLN3O4S
Molecular Weight
395.86
Exact Mass
395.071
CAS #
1024448-59-6
Related CAS #
1024448-59-6;
PubChem CID
5068295
Appearance
Off-white to light yellow solid powder
LogP
4.234
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
4
Heavy Atom Count
26
Complexity
578
Defined Atom Stereocenter Count
0
InChi Key
ZNLVYSJQUMALEO-UHFFFAOYSA-N
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
Chemical Name
1-benzyl-4-[(4-chloro-2-nitrobenzene)sulfonyl]piperazine
Synonyms
RN1747 RN 1747 RN-1747.
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 Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~126.31 mM)
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.

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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.
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 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 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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