| Dorsomorphin (Compound C)AMPK inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.59%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
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Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
| Cell experiment [1]: | |
Cell lines | HT-29 human colon cancer cells and HeLa cells, zebrafish embryos |
Preparation method | This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 40 μM, 4-10 μM, 30 min |
Applications | Dorsomorphin could inhibit AMPK activity in intact hepatocytes. Dorsomorphin inhibited autophagic proteolysis. Dorsomorphin inhibited ACC phosphorylation by 80%. Dorsomorphin inhibited proteolysis in HT-29 cells. Dorsomorphin inhibited AMPK activity in HeLa cells expressing LKB1 and STRAD and in control HeLa cells. Dorsomorphin induced dorsalization in zebrafish embryos. Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs with the IC50 of 0.47 μM. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice injected via the tail vein with 0.2 g/kg of dextran or 0.2 g/kg of iron-dextran USP, zebrafish |
Dosage form | Intraperitoneal injection, 10 mg/kg |
Application | Dorsomorphin reduced hepatic hepcidin mRNA levels to one-third of that of vehicle-injected mice. Administration of dorsomorphin over 24 h led to a 60% increase in total serum iron concentrations. Injection of dorsomorphin in mice abolished the iron-mediated increase in hepatic SMAD1/5/8 phosphorylation. Intraperitoneal injection of iron-dextran in adult zebrafish led to a nearly three-fold increase in SMAD1/5/8 phosphorylation in liver extracts within 1 h. Coinjected with iron-dextran and dorsomorphin decreased SMAD1/5/8 phosphorylation by nearly three-fold relative to fish injected with iron-dextran and vehicle. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Meley D, Bauvy C, Houben-Weerts J H P M, et al. AMP-activated protein kinase and the regulation of autophagic proteolysis[J]. Journal of biological chemistry, 2006, 281(46): 34870-34879. [2]. Paul B Y, Hong C C, Sachidanandan C, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism[J]. Nature chemical biology, 2008, 4(1): 33-41. | |
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| Cas No. | 866405-64-3 | SDF | Download SDF |
| Synonyms | Compound C | ||
| Chemical Name | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine | ||
| Canonical SMILES | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 | ||
| Formula | C24H25N5O | M.Wt | 399.49 |
| Solubility | ≥8.49 mg/mL in DMSO with ultrasonic and warming, <1.96 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Dorsomorphin is a cell-permeable and reversible ATP-competitive inhibitor of AMP-activated protein kinase (AMPK) with Ki value of 109nM [1].
Dorsomorphin is highly selective against AMPK over other structure related kinases such as protein kinase A, protein kinase C and Janus kinase 3. As an AMPK inhibitor, dorsomorphin is found to reverse the anti-proliferation induced by AMPK signaling in glucose-deprived mouse neural stem cells. It also shows inhibition of adipogenic differentiation in mouse 3T3-L1 fibroblasts [2].
Dorsomorphin is also reported to be an inhibitor of BMP signaling. It inhibits the phosphorylation of Smad 1/5/8, resulting in a reduction of heterotopic ossification. It also decreases the gene transcription of hepatic hepcidin and leads to increased iron levels subsequently. Moreover, the inhibition of BMP caused by dorsomorphin promotes self-renewal and neural induction of human ESC [2]
References:[1] Lu Y, Akinwumi BC, Shao Z, Anderson HD. Ligand Activation of Cannabinoid Receptors Attenuates Hypertrophy of Neonatal Rat Cardiomyocytes. J Cardiovasc Pharmacol. 2014 Jun 26. [2] Kudo T, Kanetaka H, Mizuno K, et al. Effects of the Small Molecule Dorsomorphin on Intracellular Signaling. Interface Oral Health Science 2011. Springer Japan, 2012: 131-133.
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1.我利用氯仿萃取生物碱，需要将氯仿蒸干，我做的样品有非常多份，但是每份样品很少，用的氯仿也很少，每份只用十几毫升左右，但是旋转蒸发仪的蒸发瓶好大，而且一次只能蒸发一个样，太慢了，就算蒸发完了，取出生物碱的时候也不好取，由于我做的是定量试验，所以如果取出生物碱时有残留会影响实验结果，到底怎么办啊？有没有特制的小的蒸发瓶？或者特制的可以一次接好几个蒸发容器的接口？
2.请问恒温水浴锅可不可以用来做蒸发？由于是蒸发氯仿，担心没有回收装置会导致泄露中毒的问题，但是我的量比较少，又想冒险试试，真是焦头烂额了现在，大家把那个我出出主意吧！！！！
不知道有多少这样的学生呢,其实我们做学生时也没人特意教,能用旋蒸都是很了不起的，老师不教也会主动学习,偷学或查资料
做实验常规试剂的沸点背不得很糟糕,但背得后问我为什么在旋蒸上蒸乙醇用60度,不用78度,我就吐血了
只好普及知识,借用BUCHI的介绍,这么有名的公司没人知道也是很菜的
羊毛冷凝器
2500年以前，由于巧合，希腊水手在公海上发现了羊毛冷凝器。当时，船只遇难，船员必须从盐水中获得重要的淡水。为此，他们将海水加热，并利用固定在罐子上方的羊毛将蒸汽冷凝。这种名为“羊毛冷凝器”的东西从古代广泛传播到现代，与较早的“瓷碗变体”比较，代表了一种巨大的进步。
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我用乙醇来提取，但是回收瓶中只有乙醇，那里出问题了呢？？？？
请问有什么方法可以不漏气呢？
谢谢大家！！
已经试过的方法有：电吹风烘箱
将试的方法是：超声
大家有什么好建议，谢谢了！
我们有个中药项目，需要采用乙酸乙酯萃取，有效成分分布在乙酸乙酯有机层中，现在我们采用旋转蒸发仪回收乙酸乙酯直到蒸发瓶中有效成分成蜂窝固体状才取出，但现在有一个问题，我如何判断蒸发瓶中蜂窝状固体可以刮出？目前我们实验室做的时候是根据蒸发瓶释放真空时蜂窝状固体不收缩的标准作为蒸干取出固体物的，但这个标准太粗放了，我也知道光靠旋转蒸发仪是不可能除尽有机溶剂，我们后续还有一个工艺可以除去蒸干固体残留的有机溶剂。我现在想知道有没有一些判断标准用于旋转蒸发仪固体蒸干可以取出来的标准可供参考啊？盼指教，谢谢
