A HIF-PH1, -2, and -3 inhibitor
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MK-8617

Item No. 33790

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[bis(4-methoxyphenyl)methyl]-1,6-dihydro-6-oxo-2-(3-pyridazinyl)-5-pyrimidinecarboxamide
CAS Number
1187990-87-9
Molecular Formula
C24H21N5O4
Formula Weight
443.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
231 nm
SMILES
O=C1NC(C2=CC=CN=N2)=NC=C1C(NC(C3=CC=C(C=C3)OC)C4=CC=C(C=C4)OC)=O
InChi Code
InChI=1S/C24H21N5O4/c1-32-17-9-5-15(6-10-17)21(16-7-11-18(33-2)12-8-16)27-23(30)19-14-25-22(28-24(19)31)20-4-3-13-26-29-20/h3-14,21H,1-2H3,(H,27,30)(H,25,28,31)
InChi Key
WXLPERVDMILVIF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    25 mg

    $185

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    50 mg

    $341

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    100 mg

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    Product Description

    MK-8617 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 1 (HIF-PH1), HIF-PH2, and HIF-PH3 (IC50s = 1, 1, and 14 nM, respectively).1 It is selective for HIF-PH1, -2, and -3 over the cytochrome P450 (CYP) isoforms CYP1A2, -3A4, -2B6, -2C9, -2C19, and -2D6 (IC50s = >1.6 µM for all) and factor inhibiting HIF (FIH; IC50 = 18 µM), as well as over a panel of 171 enzymes at 10 µM. MK-8617 (5 and 15 mg/kg) increases serum levels of erythropoietin (EPO) and hemoglobin, as well as the number of circulating red blood cells, in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Debenham, J.S., Madsen-Duggan, C., Clements, M.J., et al. Discovery of N-[bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia. J. Med. Chem. 59(24), 11039-11049 (2016).