A selective inhibitor of CYP3A4
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SR 9186

Item No. 13888

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4'-cyano[1,1'-biphenyl]-4-yl)-N'-[4-(3H-imidazo[4,5-b]pyridin-7-yl)phenyl]-urea
CAS Number
1361414-26-7
Molecular Formula
C26H18N6O
Formula Weight
430.5
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: SolubleDMSO: Soluble
SMILES
O=C(NC1=CC=C(C2=CC=C(C#N)C=C2)C=C1)NC3=CC=C(C4=CC=NC5=C4N=CN5)C=C3
InChi Code
InChI=1S/C26H18N6O/c27-15-17-1-3-18(4-2-17)19-5-9-21(10-6-19)31-26(33)32-22-11-7-20(8-12-22)23-13-14-28-25-24(23)29-16-30-25/h1-14,16H,(H,28,29,30)(H2,31,32,33)
InChi Key
FEDMEJWMCJAMHE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $568

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    Product Description

    SR 9186 is an inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 0.011 µM).1 It is highly selective for CYP3A4 over CYP3A5 (IC50 = 33 µM). SR 9186 inhibits metabolism of midazolam to 1’-hydroxy midazolam, testosterone to 6β-hydroxy testosterone, and vincristine to vincristine M1 in isolated human liver microsomes (HLMs) expressing recombinant CYP3A4 (IC50s = 9, 4, and 38 nM, respectively) but not microsomes expressing recombinant CYP3A5.2 It decreases lapatinib-induced quinoneimine-glutathione adduct formation in HLMs by 78% when used at a concentration of 2.5 µM.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Song, X., Li, X., Ruiz, C.H., et al. Imidazopyridines as selective CYP3A4 inhibitors. Bioorg. Med. Chem. Lett. 22(4), 1611-1614 (2012).

    2. Li, X., Song, X., Kamenecka, T.M., et al. Discovery of a highly selective CYP3A4 inhibitor suitable for reaction phenotyping studies and differentiation of CYP3A4 and CYP3A5. Drug Metab. Dispos. 40(9), 1803-1809 (2012).

    3. Towles, J.K., Clark, R.N., Wahlin, M.D., et al. Cytochrome P450 3A4 and CYP3A5-catalyzed bioactivation of lapatinib. Drug Metab. Dispos. 44(10), 1584-1597 (2016).