A pan HIF-PH inhibitor
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TP-0463518

Item No. 33788

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-1,2,5,6-tetrahydro-4-hydroxy-2-oxo-3-pyridinyl]carbonyl]-glycine
CAS Number
1558021-37-6
Molecular Formula
C20H18ClN3O6
Formula Weight
431.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 25 mg/ml
λmax
231, 274 nm
SMILES
O=C(CNC(C1=C(O)CCN(CC2=CN=C(C=C2)OC3=CC=C(C=C3)Cl)C1=O)=O)O
InChi Code
InChI=1S/C20H18ClN3O6/c21-13-2-4-14(5-3-13)30-16-6-1-12(9-22-16)11-24-8-7-15(25)18(20(24)29)19(28)23-10-17(26)27/h1-6,9,25H,7-8,10-11H2,(H,23,28)(H,26,27)
InChi Key
HMMHKGLPKAQOOH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $53

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    10 mg

    $98

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    25 mg

    $194

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    50 mg

    $332

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    Product Description

    TP-0463518 is a pan hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor.1 It inhibits human HIF-PH1 (Ki = 5.3 nM), as well as human HIF-PH2 and HIF-PH3 (IC50s = 18 and 63 nM, respectively). TP-0463518 (5 mg/kg) increases serum levels of erythropoietin (EPO) in mice. It also increases serum EPO levels in a 5/6 nephrectomy-induced rat model of chronic kidney disease when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kato, S., Takayama, N., Takano, H., et al. TP0463518, a novel inhibitor for hypoxia-inducible factor prolyl hydroxylases, increases erythropoietin in rodents and monkeys with a good pharmacokinetics-pharmacodynamics correlation. Eur. J. Pharmacol. 838, 138-144 (2018).