貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S82275-5mg	99.9%	￥600.00 S82275-5mg ￥600.00 現(xiàn)貨	6 6	-	-	-
S82275-10mg	99.9%	￥1000.00 S82275-10mg ￥1000.00 現(xiàn)貨	6 6	-	-	-
S82275-25mg	99.9%	￥2000.00 S82275-25mg ￥2000.00 現(xiàn)貨	6 6	-	-	-

產(chǎn)品介紹

JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.

產(chǎn)品描述：

JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.

靶點(diǎn)：

pKi: 7.91±0.04 (PHD1), 7.29 ±0.05 (PHD2), 7.65±0.09(PHD3);HIF/HIFProlyl-Hydroxylase

體外研究：

JNJ-42041935 is the most potent inhibitor of PHD2181–417with 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)

體內(nèi)研究：

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

參考文獻(xiàn)：

1. Barrett TD, et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Mol Pharmacol. 2011 Jun;79(6):910-20.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.885 ml	14.424 ml	28.848 ml
5 mM	0.577 ml	2.885 ml	5.77 ml
10 mM	0.288 ml	1.442 ml	2.885 ml
50 mM	0.058 ml	0.288 ml	0.577 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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