1558021-37-6
Chemical Structure
TP0463518
- CAS. Nr.: 1558021-37-6
- Formula:C20H18ClN3O6
- Molecular Weight:431.83
IUPAC Name: (1-((6-(4-chlorophenoxy)pyridin-3-yl)methyl)-4-hydroxy-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
InChIKey: HMMHKGLPKAQOOH-UHFFFAOYSA-N
SMILES: ClC(C=C1)=CC=C1OC2=NC=C(CN3C(C(C(NCC(O)=O)=O)=C(O)CC3)=O)C=C2
Biological Activity: TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3. TP0463518 competitively inhibits human PHD1 (IC50=18 nM), PHD2 (Ki=5.3 nM), and PHD3 (IC50=63 nM), and targets monkey PHD2 with an IC50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia[1][2].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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TP0463518 | 99.25% | TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3. TP0463518 competitively inhibits human PHD1 (IC50=18 nM), PHD2 (Ki=5.3 nM), and PHD3 (IC50=63 nM), and targets monkey PHD2 with an IC50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia. | ||||||||||||||||||||
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References
- [1]. Kato S, 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. 2018 Nov 5;838:138-144. [Content Brief]
- [2]. Kato S, et al. TP0463518 (TS-143) Ameliorates Peptidoglycan-Polysaccharide Induced Anemia of Inflammation in Rats. Biol Pharm Bull. 2021;44(11):1653-1661. [Content Brief]
