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嘌吗啡胺

嘌吗啡胺用途

Purmorphamine是一种平滑受体激动剂,EC50为1 μM。

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嘌吗啡胺名称

[ CAS 号 ]:
483367-10-8

[ 中文名 ]:
嘌吗啡胺

[ 英文名 ]:
Purmorphamine

[英文别名 ]:

Purmorphamine

嘌吗啡胺生物活性

[ 描述 ]:

Purmorphamine是一种平滑受体激动剂,EC50为1 μM。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 干细胞及 Wnt 通路 >> SMO

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 1.5 μM (Smoothened)

[体外研究]

根据MTT测定,Purmorphamine(10,20μM)与西罗莫司组合显着降低细胞数量。在第14天,Purmorphamine诱导碱性磷酸酶活性和RUNX-2表达的上调。诱导后第14天在3和5μM剂量的嘌呤胺上检测到骨钙蛋白的上调。在存在或不存在嘌吗啡胺的情况下,基质矿化保持不变[1]。 Purmorphamine诱导小鼠ES细胞系ES14和间充质干细胞系C3H10T1/2中的STAT3磷酸化[2]。 Purmorphamine上调人骨髓间充质细胞中成骨细胞表型-ALP活性和骨样结节形成标志物的表达[3]。

[细胞实验]

为了确定小分子的无毒剂量，将5×105个传代-3的人MSC接种在六孔培养板的每个孔中，并在37℃，5％CO 2下在扩增培养基（如上所述）中温育。两天后，将培养基更换为成骨培养基（OM），其由补充有10％FBS，10nM地塞米松，50μg/ mL抗坏血酸2-磷酸和10mMβ-甘油磷酸的α-MEM组成。该OM补充有不同浓度的嘌吗啡胺（1,3,5,10和20μM）和西罗莫司（0.1,1,10,100和200nM）。将培养物再保持2天，然后通过MTT测定，通过以1：5的比例向培养基中加入MTT溶液（PBS中5mg / mL）评估活细胞的存在。然后将细胞在37℃和5％CO 2下孵育。两小时后，除去培养基并向处理过的细胞中加入500μLDMSO以溶解形成区沉淀。在570nm处读取光学吸收率。细胞活力计算为相对于仅用OM处理的对照组的百分比值。

[参考文献]

[1]. F. Faghihia, et al. The effect of purmorphamine and sirolimus on osteogenic differentiation of human bone marrow-derived mesenchymal stem cells. Biomedicine & Pharmacotherapy. 2013, 67(1): 31-38.

[2]. Gu D, et al. A role for transcription factor STAT3 signaling in oncogene smoothened-driven carcinogenesis. J Biol Chem. 2012 Nov 2;287(45):38356-66.

[3]. Beloti MM, et al. Purmorphamine enhances osteogenic activity of human osteoblasts derived from bone marrow mesenchymal cells. Cell Biol Int. 2005 Jul;29(7):537-41.

[相关活性小分子]

嘌吗啡胺物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
790.3±70.0 °C at 760 mmHg

[ 熔点 ]:
210-212ºC

[ 分子式 ]:
C₃₁H₃₂N₆O₂

[ 分子量 ]:
520.625

[ 闪点 ]:
431.8±35.7 °C

[ 精确质量 ]:
520.258667

[ PSA ]:
77.33000

[ LogP ]:
4.52

[ 外观性状 ]:
white to beige

[ 蒸汽压 ]:
0.0±2.8 mmHg at 25°C

[ 折射率 ]:
1.711

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
DMSO: soluble5mg/mL, clear (warmed)

嘌吗啡胺MSDS

详细MSDS(安全技术说明书)

嘌吗啡胺安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

嘌吗啡胺文献

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