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TP-0463518 is a pan hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. 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.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: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml, DMSO: 25 mg/ml. lambdamax: 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.
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