JNJ 303 is a potent voltage-dependent IKs-channel blocker encoded by KCNQ1/KCNE1 with an IC50 value of 64 nM. JNJ 303 induces Q-T prolongation and causes torsades de pointes (TdP).

 

Brand: BCM

 

Target: Potassium Channel

 

Signaling Pathways: Membrane transporter/Ion channel

 

In Vitro: Optical mapping was used to measure action potential durations (APDs) in the presence of the IKs blocker JNJ-303 and the IKr blocker E-4031.?JNJ-303 alone did not increase APD.?However, under isoprenaline (ISO), both the application of JNJ-303 and additional E-4031 significantly increased APD.?With JNJ-303, ISO decreased APD significantly more in the epicardium as compared to the endocardium, with subsequent application E-4031 increasing mid- and endocardial APD80 more significantly than in the epicardium.?We found that β-AR stimulation significantly augmented the effect of IKs blocker JNJ-303, in contrast to the reduced effect of IKr blocker E-4031.

 

pKa: 10.63±0.40(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: CC(C)(C(=O)NC1[C@@H]2CC3C[C@H]1CC(C2)(C3)NS(=O)(=O)C)OC4=CC=C(C=C4)Cl  

 

InChIKey: OSGIRCJRKSAODN-DJASPMHUSA-N  

 

InChI: InChI=1S/C21H29ClN2O4S/c1-20(2,28-17-6-4-16(22)5-7-17)19(25)23-18-14-8-13-9-15(18)12-21(10-13,11-14)24-29(3,26)27/h4-7,13-15,18,24H,8-12H2,1-3H3,(H,23,25)/t13?,14-,15+,18?,21?

 

Attribute
[Chem Name]	2-(4-chlorophenoxy)-N-[(1S,3R)-5-(methanesulfonamido)-2-adamantyl]-2-methylpropanamide
[Synonym]	JNJ 303
[CAS No.]	878489-28-2
[MDL No.]	MFCD18086905
[Formula]	C21H29ClN2O4S
[Molecular]	440.98
[Form]	Solid Powder
[Storage]	Sealed in dry, 2-8°C

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