A PDE4D negative allosteric modulator
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D159687

Item No. 38778

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(3′-chloro-6-methoxy[1,1′-biphenyl]-3-yl)methyl]phenyl]-urea
CAS Number
1155877-97-6
Molecular Formula
C21H19ClN2O2
Formula Weight
366.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 10 mg/ml
λmax
246 nm
SMILES
O=C(NC1=CC=C(CC2=CC=C(C(C3=CC(Cl)=CC=C3)=C2)OC)C=C1)N
InChi Code
InChI=1S/C21H19ClN2O2/c1-26-20-10-7-15(12-19(20)16-3-2-4-17(22)13-16)11-14-5-8-18(9-6-14)24-21(23)25/h2-10,12-13H,11H2,1H3,(H3,23,24,25)
InChi Key
RJJLUTWHJUDZFP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $104

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    25 mg

    $228

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    Product Description

    D159687 is a negative allosteric modulator of phosphodiesterase 4D (PDE4D; IC50 = 28 nM for the human enzyme).1 It is selective for PDE4D over PDE4B (IC50 = 562 nM for the human enzyme), as well as 14 other PDE isoforms (IC50s = >1.4 µM). D159687 decreases forskolin-induced cAMP hydrolysis in HEK293 cells (IC50 = 253 nM) and dextran gel-induced increases in leukotriene E4 production in isolated human whole blood (IC50 = 44 nM). It impairs novel object recognition in mice when administered at a dose of 3 mg/kg but does not increase anesthesia duration, a proxy measure of emesis induction, in mice at 3 or 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burgin, A.B., Magnusson, O.T., Singh, J., et al. Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety. Nat. Biotechnol. 28(1), 63-70 (2010).

    2. Zhang, C., Xu, Y., Zhang, H.-T., et al. Comparison of the Pharmacological Profiles of Selective PDE4B and PDE4D Inhibitors in the Central Nervous System. Sci. Rep. 7, 40115 (2017).