货号:A137399
同义名:
Compound C; BML-275
Dorsomorphin is a selective AMPK inhibitor with Ki value of 109 nM.
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产品名称 | AMPK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
WZ4003 |
++++
NUAK1, IC50: 20 nM NUAK2, IC50: 100 nM |
98+% | |||||||||||||||||
Dorsomorphin |
++
AMPK, Ki: 109 nM |
99% | |||||||||||||||||
HTH-01-015 |
+++
NUAK1 , IC50: 100 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Dorsomorphin, known as compound C, is a reversible selective ATP-competitive inhibitor of AMPK with Ki of 109 nM. Dorsomorphin can also inhibit the bone morphogenic protein (BMP) signaling and do not effect the expression of several structurally related kinases including ZAPK, SYK, PKCq, PKA, and JAK3[3]. In addition, dorsomorphin could stimulate the oxidation of long chain fatty acids independently in adipocytes by increasing carnitine palmitoyltransferase-1 (CPT1) activity[4] and remarkly reduce the adipogenic Differentiation of 3T3-L1 cells at 10 μM[5]. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway[6]. In vivo, dorsomorphin induces dorsalization in zebrafish embryos and the differentiation of osteoblast[7]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
mouse C2C12 cells | 4 μM | Function assay | Inhibition of BMPR1-mediated osteoblast differentiation in BMP4-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry | 18026094 |
Dose | Mice: 3 mg/kg - 12 mg/kg[3] (i.p.) Rat: 0.2 mg/kg[4] (i.v.) |
Administration | i.p., i.v. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.50mL 0.50mL 0.25mL |
12.52mL 2.50mL 1.25mL |
25.03mL 5.01mL 2.50mL |
CAS号 | 866405-64-3 |
分子式 | C24H25N5O |
分子量 | 399.49 |
SMILES Code | C(CN1CCCCC1)OC1=CC=C(C=C1)C1=CN2N=CC(=C2N=C1)C1=CC=NC=C1 |
MDL No. | MFCD08705402 |
别名 | Compound C; BML-275 |
运输 | 蓝冰 |
InChI Key | XHBVYDAKJHETMP-UHFFFAOYSA-N |
Pubchem ID | 11524144 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,2-8°C |
溶解方案 |
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。
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动物实验配方 |
IP 2% DMSO+water 0.04 mg/mL clear PO 0.5% CMC-Na 55 mg/mL suspension |