货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S55211-1ml促销	10mM in DMSO	￥720.00 ￥570.00 S55211-1ml ￥570.00 现货	10 10	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S55211-1ml促销

10mM in DMSO

￥720.00 ￥570.00

产品描述：

PORCN抑制剂;PORCN Inhibitors;;InformationGNF-6231 GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.TargetsPorcupine (Cell-free) 0.8 nMIn vitroGNF-6231 shows a good solubility. It has no appreciable activities, at least up to 10 μM testing concentrations, for more than 200 off-targets, which include GPCRs, kinases, proteases, transporters, ion channels, and nuclear receptors. GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested (2C9, 2D6, 3A4). It shows high permeability in a Caco-2 human cell permeability assay with a possible efflux.In vivoGNF-6231 demonstrates excellent pathway inhibition and induces robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model. GNF-6231 is moderately bound to mouse, rat, dog, monkey, and human plasma proteins (88.0, 83.1, 90.9, 71.2, and 95%, respectively). It shows good oral bioavailability, ranging from 72 to 96% in preclinical species (mouse, rat, and dog) when dosed in solution formulations. GNF-6231 is expected to have minimal to marginal distribution to tissues compared to total body water following intravenous administration to mouse (Vss 0.57 L/kg), rat (Vss 0.70 L/kg), and dog (Vss 0.25 L/kg).Cell Research(from reference)Cell lines：TM3 Wnt-Luc cells and L-cell Wnt3A cells Incubation Time：24 h

体内研究：

GNF-6231 (5 mg/kg; 静脉注射; 每 24 h 一次，连续 6 天) 在发生心肌梗死的 C57Bl/6 小鼠中通过抑制 Wnt 通路的激活来缓解心机梗死的症状。
GNF-6231 (0.3-3 mg/kg; 口服; 一天一次连续两周) 在 MMTV-WNT1 异种移植肿瘤小鼠中具有抗肿瘤活性。

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.23 ml	11.149 ml	22.297 ml
5 mM	0.446 ml	2.23 ml	4.459 ml
10 mM	0.223 ml	1.115 ml	2.23 ml
50 mM	0.045 ml	0.223 ml	0.446 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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