RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity over related TRP receptors such as TRPV1, TRPV3, and TRPM8. RN-1665 can be used for focused screens of TRPV4 probes with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively.

Physicochemical Properties

Molecular Formula	C20H24F5N3O3S2
Molecular Weight	513.54
CAS #	1803003-65-7
Appearance	Solid powder
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

Targets	hTRPV4 0.26 μM (IC50) rTRPV4 0.39 μM (IC50)
References	[1]. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (194.73 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (4.87 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make it 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 (4.87 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well. *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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.9473 mL	9.7363 mL	19.4727 mL
	5 mM	0.3895 mL	1.9473 mL	3.8945 mL
	10 mM	0.1947 mL	0.9736 mL	1.9473 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.