An inhibitor of HIF-PH
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Desidustat

Item No. 28074

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[1-(cyclopropylmethoxy)-1,2-dihydro-4-hydroxy-2-oxo-3-quinolinyl]carbonyl]-glycine
CAS Number
1616690-16-4
Molecular Formula
C16H16N2O6
Formula Weight
332.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3mg/mlDMSO: 3mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5mg/mlEthanol: 1mg/ml
λmax
233, 291, 335
SMILES
O=C1C(C(NCC(O)=O)=O)=C(O)C2=CC=CC=C2N1OCC3CC3
InChi Code
InChI=1S/C16H16N2O6/c19-12(20)7-17-15(22)13-14(21)10-3-1-2-4-11(10)18(16(13)23)24-8-9-5-6-9/h1-4,9,21H,5-8H2,(H,17,22)(H,19,20)
InChi Key
IKRKQQLJYBAPQT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    10 mg

    $160

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    50 mg

    $558

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    100 mg

    $796

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    Product Description

    Desidustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH).1 It reduces levels of hypoxia-inducible factor-1α (HIF-1α), a transcription factor regulated by HIF-PH enzymes, in rat liver and kidney. Desidustat increases the expression of the red blood cell- and iron transport-related genes Epo, Fpn1, and Hamp in rat liver in a model of anemia induced by peptidoglycan-polysaccharide (PGPS).2 It increases plasma levels of erythropoietin in rats by 10.3- to 40-fold when administered at doses of 15 and 30 mg/kg, respectively.1 Desidustat (15 and 30 mg/kg) also increases plasma levels of erythropoietin and hemoglobin, as well as the number of circulating red blood cells, in nephrectomized rats in a model of chronic kidney disease-induced anemia. It increases hemoglobin levels and the number of circulating red blood cells in a mouse model of anemia induced by the DNA-crosslinking agent cisplatin (Item No. 13119).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jain, M.R., Joharapurkar, A.A., Pandya, V., et al. Pharmacological characterization of ZYAN1, a novel prolyl hydroxylase inhibitor for the treatment of anemia. Drug Res. (Stuttg.) 66(2), 107-112 (2016).

    2. Jain, M., Joharapurkar, A., Patel, V., et al. Pharmacological inhibition of prolyl hydroxylase protects against inflammation-induced anemia via efficient erythropoiesis and hepcidin downregulation. Eur. J. Pharmacol. 843, 113-120 (2019).