货号	规格	价格	上海	北京	珠海	重庆	武汉
S88000-5mg促销	≥98%	￥262.00 ￥235.00 S88000-5mg ￥235.00 现货	7 7	-	-	-	-
S88000-10mg促销	≥98%	￥466.00 ￥420.00 S88000-10mg ￥420.00 现货	6 6	-	-	-	-
S88000-25mg促销	≥98%	￥580.00 ￥522.00 S88000-25mg ￥522.00 现货	2 2	-	-	-	-
S88000-50mg促销	≥98%	￥1010.00 ￥914.00 S88000-50mg ￥914.00 现货	2 2	-	-	-	-
S88000-100mg促销	≥98%	￥1720.00 ￥1550.00 S88000-100mg ￥1550.00 现货	2 2	-	-	-	-

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产品描述：

MK-8617是一种具有口服活性的Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3)泛抑制剂，抑制PHD1, 2, 3 的IC50s分别为1.0, 1.0 和 14 nM

靶点：

PHD1(Cell-free assay):1 nM;PHD2(Cell-free assay):1 nM;PHD3(Cell-free assay):14 nM;HIF/HIFProlyl-Hydroxylase

体内研究：

Tritiated MK-8617 exhibited minimal metabolic turnover in liver microsomes (+NADPH) from rat, dog, and monkey (<10% turover) but significant turnover in human liver microsomes (34% turnover) after 60 min (10 μM compound, 1 mg/mL microsomal protein). In terms of its pharmacokinetic profile, MK-8617 showed good oral bioavailability across species (36−71%), with low clearance and volume of distribution. The compound still has a relatively long elimination half-life across preclinical species. In mice (C57Bl/6), single doses of 5 and 15 mpk po (n = 3) caused increases in circulating reticulocytes measured on both 3 and 4 days postcompound challenge. In rat (Sprague−Dawley), a single dose titration of 1.5, 5, and 15 mpk po (n = 5) caused a large increase in serum erythropoietin(EPO) levels of 1.7-, 8-, and 204-fold relative to vehicle, respectively. Increases in circulating reticulocytes are observed at 5 and 15 mg/kg 3 days after challenge and, with the 15 mg dose, at 4 days after challenge

细胞实验：

Cell lines: HEK293 cells Concentrations: 15 & 30 μM Incubation Time: 24 h Method: Cells were treated with various concentrations of MK-8617.

动物实验：

Animal Models: C57Bl/6 mice Dosages: 1 mg/kg po, 0.5 mg/kg iv Administration: i.v 或 p.o

参考文献：

1. John S. Debenham, et al. J Med Chem. 2016, 59 (24):11039-11049. 2. Sulser P, et al. FASEB J. 2020 Feb;34(2):2344-2358.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.255 ml	11.275 ml	22.55 ml
5 mM	0.451 ml	2.255 ml	4.51 ml
10 mM	0.226 ml	1.128 ml	2.255 ml
50 mM	0.045 ml	0.226 ml	0.451 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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