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JNJ-42041935

CAS No. : 1193383-09-3

MCE 国际站：JNJ-42041935

产品活性：JNJ-42041935是高效的，竞争性和选择性的脯氨酰羟化酶PHD抑制剂，抑制PHD1，PHD2 和 PHD3的pK_i值分别为7.91±0.04，7.29 ±0.05和7.65±0.09。

研究领域：Metabolic Enzyme/Protease

作用靶点：HIF/HIF Prolyl-Hydroxylase

In Vitro: JNJ-42041935 is the most potent inhibitor of PHD2_181–417 with a pIC₅₀ value of 7.0±0.03. JNJ-42041935 also inhibits full-length PHD1, PHD2, andPHD3 enzymes (pK_i values 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively) .

In Vivo: JNJ-42041935 is used to compare the effect of selective inhibition of PHD to intermittent, high doses (50 μg/kg i.p.) of an exogenous erythropoietin receptor agonist in an inflammation induced anemia model in rats. JNJ-42041935 (100 μmol/kg, once a day for 14 days) is effective in reversing inflammation induced anemia, whereas erythropoietin has no effect. Administration of JNJ-42041935 (100 μmol/kg p.o.) for 5 consecutive days resulted in a 2-fold increase in reticulocytes, an increase in hemoglobin by 2.3 g/dl, and an increase in the hematocrit of 9%. Two hours after oral administration of 300 μmol/kg JNJ-42041935, the bioluminescence over the peritoneal area is increased by 2.2 ± 0.3-fold relative to luciferase-treated vehicle controls in the mouse .

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