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JNJ-42041935
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JNJ-42041935
CAS No. : 1193383-09-3
MCE 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pKi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 PHD2181–417 with a pIC50 value of 7.0±0.03. JNJ-42041935 also inhibits full-length PHD1, PHD2, and PHD3 enzymes (pKi 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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