JNJ 303

Catalog No.S0087 Batch:S008701

Technical Data

Formula	C₂₁H₂₉ClN₂O₄S
Molecular Weight	440.98	CAS No.	878489-28-2
Solubility (25°C)*	In vitro	DMSO	88 mg/mL (199.55 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

JNJ 303 is a potent blocker of the voltage dependent I_Ks-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).

Targets

I_Ks-channel ^[1]
(Cell-free assay)

64 nM

In vitro

JNJ 303 induces a decrease in I_CaL, which is more pronounced in atrial cells compared to ventricular cells.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines murine atrial and ventricular cells Concentrations 1 μM, 70 nM Incubation Time -- Method The cells were incubated with 10 μM Isoproterenol (ISO), dissolved in IMDM with 20 % FBS, at 37℃ for 1-2 hours, prior to the measurement of APs in the whole cell mode. For recording of the ICaL, β-adrenergic stimulation was accomplished via perfusion of the cells with external solution containing 10 μM ISO. Further drug administration (JNJ 303) was done via the gravitational perfusion system. APs and currents were recorded in whole cell mode.

Cell Assay:^{^[1]}

Cell lines
murine atrial and ventricular cells
Concentrations
1 μM, 70 nM
Incubation Time
--
Method
The cells were incubated with 10 μM Isoproterenol (ISO), dissolved in IMDM with 20 % FBS, at 37℃ for 1-2 hours, prior to the measurement of APs in the whole cell mode. For recording of the ICaL, β-adrenergic stimulation was accomplished via perfusion of the cells with external solution containing 10 μM ISO. Further drug administration (JNJ 303) was done via the gravitational perfusion system. APs and currents were recorded in whole cell mode.

References

[1] Julie Albrecht. FINAL_Thesis. Feb. 2017

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