A modulator of CFTR
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IOWH-032

Item No. 30273

Technical Information
Formal Name
3-(3,5-dibromo-4-hydroxyphenyl)-N-[(4-phenoxyphenyl)methyl]-1,2,4-oxadiazole-5-carboxamide
CAS Number
1191252-49-9
Molecular Formula
C22H15Br2N3O4
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
218 nm
SMILES
O=C(C1=NC(C2=CC(Br)=C(O)C(Br)=C2)=NO1)NCC(C=C3)=CC=C3OC4=CC=CC=C4
InChi Code
InChI=1S/C22H15Br2N3O4/c23-17-10-14(11-18(24)19(17)28)20-26-22(31-27-20)21(29)25-12-13-6-8-16(9-7-13)30-15-4-2-1-3-5-15/h1-11,28H,12H2,(H,25,29)
InChi Key
DSFNLJXHXBIKDS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    IOWH-032 is a modulator of the cystic fibrosis transmembrane conductance regulator (CFTR).1,2 It inhibits CFTR in T84 human colon cells (IC50 = 8.51 µM).1 It has rapid inhibitory and slow potentiating effects on human CFTR with apparent Kd values of 6.1 and 0.64 nM, respectively.2 IOWH-032 (20 nM) also potentiates currents through CFTR bearing the F508 deletion mutation (ΔF508-CFTR) expressed in X. laevis oocytes. It inhibits, but does not potentiate, mouse CFTR with an apparent Kd value of 42.9 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Doyle, K.J., Jones, G.P., Russell, M.G.N., et al. Compounds, compositions and methods compromising heteroaromatic derivates. US2009/0318429Al, (2009).

    2. Cui, G., Khazanov, N., Stauffer, B.B., et al. Potentiators exert distinct effects on human, murine, and Xenopus CFTR. Am. J. Physiol. Lung. Cell. Mol. Physiol. 311(2), L192-207 (2016).