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).

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)

Biological Activity

References

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

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. 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.