货号	规格	价格	上海	北京	珠海	重庆	武汉
S88425-5mg买3赠1	99.10%	￥600.00 S88425-5mg ￥600.00 现货（买3赠1）	6 6	-	-	-	-
S88425-10mg促销	99.10%	￥1000.00 ￥800.00 S88425-10mg ￥800.00 现货	6 6	-	-	-	-
S88425-25mg促销	99.10%	￥1900.00 ￥1520.00 S88425-25mg ￥1520.00 现货	5 5	-	-	-	-
S88425-50mg促销	≥98%	￥2800.00 ￥2240.00 S88425-50mg ￥2240.00 2-3天	0 货期：2-3天	-	-	-	-
S88425-100mg促销	≥98%	￥4800.00 ￥3840.00 S88425-100mg ￥3840.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

TP-0463518 is a highly potent HIF prolyl hydroxylase (PHD) inhibitor (IC50s: 13 nM and 18 nM for human and rat PHD2, respectively).

靶点：

HIF/HIF Prolyl-Hydroxylase;HIF/HIFProlyl-Hydroxylase

体内研究：

In normal mice and rats, TP0463518 significantly increased the serum EPO levels at doses of 5 and 20mg/kg, respectively. TP0463518 also increased the serum EPO level in 5/6 nephrectomized chronic kidney disease model rats at a dose of 10mg/kg, with a correlation factor for serum EPO and the serum TP0463518 levels of 0.82. TP0463518 was promptly removed with a half-life of 5.2h and increased the area under the curve (AUC) of EPO at a dose of 5mg/kg.

动物实验：

Nine-week-old Balb/c mice were randomly assigned to a vehicle or a 5 to 40 mg/kg dose of TP0463518 group. The mice were orally treated with 0.5% methylcellulose or a TP0463518 dosing suspension. Blood was collected at 6 h after administration from the orbital plexus under deep anesthesia, and euthanasia was performed without awakening. An aliquot of blood was mixed with EDTA, and the remaining blood sample was left to stand at room temperature for 15 min. The samples were then centrifuged (2130 x g for 10 min at 4°C) to prepare the plasma and serum.

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.316 ml	11.579 ml	23.157 ml
5 mM	0.463 ml	2.316 ml	4.631 ml
10 mM	0.232 ml	1.158 ml	2.316 ml
50 mM	0.046 ml	0.232 ml	0.463 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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