产品
编 号：F088350
分子式：C24H25FN6O2
分子量：448.49
分子式：C24H25FN6O2
分子量：448.49
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1243245-18-2
产品详情
生物活性：
GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.
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。Animal Model:C57Bl/6 mice model of myocardial infarction
Dosage:5 mg/kg
Administration:Intravenous injection (i.v.); Starting from 6 hours after myocardial infarction surgery to the sixth day after infarction, once every 24 hours
Result:Reduced nuclear and cytoplasmic β-catenin levels.Reduced adverse cardiac remodeling and reduced myocardial infarction area in mice (9.07%).Enhanced the overall heart repair and recovery after left ventricular infarction.
Animal Model:Mouse MMTV-WNT1 xenograft tumor model
Dosage:0.3 mg/kg,1.0 mg/kg, 3 mg/kg
Administration:Oral gavage; Once daily for 2 weeks
Result:At a single dose of 3 mg/kg, reduced the level of Wnt target gene Axin2 mRNA.Promoted tumor regression in mice in a dose-dependent manner.
体外研究：
GNF-6231 能抑制 Porcupine 酶的活性 IC50 为 0.8 nM，且在 20 μM 的浓度范围内不具有细胞毒性。
GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.
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。Animal Model:C57Bl/6 mice model of myocardial infarction
Dosage:5 mg/kg
Administration:Intravenous injection (i.v.); Starting from 6 hours after myocardial infarction surgery to the sixth day after infarction, once every 24 hours
Result:Reduced nuclear and cytoplasmic β-catenin levels.Reduced adverse cardiac remodeling and reduced myocardial infarction area in mice (9.07%).Enhanced the overall heart repair and recovery after left ventricular infarction.
Animal Model:Mouse MMTV-WNT1 xenograft tumor model
Dosage:0.3 mg/kg,1.0 mg/kg, 3 mg/kg
Administration:Oral gavage; Once daily for 2 weeks
Result:At a single dose of 3 mg/kg, reduced the level of Wnt target gene Axin2 mRNA.Promoted tumor regression in mice in a dose-dependent manner.
体外研究：
GNF-6231 能抑制 Porcupine 酶的活性 IC50 为 0.8 nM，且在 20 μM 的浓度范围内不具有细胞毒性。
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