A TRPV4 channel antagonist
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GSK2193874

Item No. 17715

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
CAS Number
1336960-13-4
Molecular Formula
C37H38BrF3N4O
Formula Weight
691.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 14 mg/mlEthanol: 15 mg/mlEthanol:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
209, 241, 330 nm
SMILES
BrC1=CC=C(C(C(NC2(CC2)C3=CC=CC=C3)=O)=C(CN4CCC(N5CCCCC5)CC4)C(C6=CC=CC(C(F)(F)F)=C6)=N7)C7=C1
InChi Code
InChI=1S/C37H38BrF3N4O/c38-28-12-13-30-32(23-28)42-34(25-8-7-11-27(22-25)37(39,40)41)31(24-44-20-14-29(15-21-44)45-18-5-2-6-19-45)33(30)35(46)43-36(16-17-36)26-9-3-1-4-10-26/h1,3-4,7-13,22-23,29H,2,5-6,14-21,24H2,(H,43,46)
InChi Key
UIVOZBSCHXCGPS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $203

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    25 mg

    $436

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    Product Description

    GSK2193874 is a potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC50 values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively.1 It is selective for TRPV4 over ~200 other human receptors, channels, and enzymes. GSK2193874 is effective in vivo, as it resolves pulmonary edema resulting from myocardial infarction in mice.1 TRPV4 blockade with GSK2193874 does not alter heart rate or blood pressure in rats, although it attenuates decreases in pulmonary and systemic arterial pressures induced by TRPV4 agonists.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thorneloe, K.S., Cheung, M., Bao, W., et al. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci. Transl. Med. 4(159), (2012).

    2. Pankey, E.A., Kassan, M., Choi, S.K., et al. Vasodilator responses to acetylcholine are not mediated by the activation of soluble guanylate cyclase or TRPV4 channels in the rat. Am. J. Physiol. Heart Circ. Physiol. 306(11), 1495-1506 (2014).