An inhibitor of Kv7.1
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JNJ-303

Item No. 37345

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(4-chlorophenoxy)-2-methyl-N-[5-[(methylsulfonyl)amino]tricyclo[3.3.1.13,7]dec-2-yl]-propanamide, stereoisomer
CAS Number
878489-28-2
Molecular Formula
C21H29ClN2O4S
Formula Weight
441.0
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlEthanol: insolPBS (pH 7.2): insol
λmax
225 nm
SMILES
O=C(C(C)(C)OC(C=C1)=CC=C1Cl)N[C@@H]([C@@H]2C3)[C@H](C[C@@H]4C2)C[C@@]3(C4)N[S](C)(=O)=O
InChi Code
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-
InChi Key
OSGIRCJRKSAODN-HPMFMUNCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $43

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    JNJ-303 is an inhibitor of voltage-gated potassium channel Kv7.1 (IC50 = 0.064 µM).1 It is selective for inhibiting Kv7.1 currents (IKs) over INa, IKr, Ito, IK1, and ICaL (IC50s =3.3, 12.6, 11.1, >100, and >10 µM, respectively). It selectively inhibits the heteromeric Kv7.1-KCNE1 complex (IC50 = 0.0784 µM) with no effect on homomeric Kv7.1, Kv7.2, or Kv1.5 in Xenopus oocytes at 1 µM.2 JNJ-303 prolongs the QT interval and also induces pause-dependent torsade de pointes (TdP) in anesthetized dogs when used at doses of 0.63 and 1.25 mg/kg, respectively.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Towart, R., Linders, J.T.M., Herman, A.N., et al. Blockade of the IKS potassium channel: An overlooked cardiovascular liability in drug safety screening? J. Pharmacol. Toxicol. Methods 60(1), 1-10 (2009).

    2. Wrobel, E., Rothenberg, I., Krisp, C., et al. KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting. Nat. Commun. 7, 12795 (2016).