Cardiogenol C hydrochloride|1049741-55-0|-陌孚医药/Medlife

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Cardiogenol C hydrochloride

目录号: PC15891 纯度: ≥98%

CAS No. :1049741-55-0

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中文名称	Cardiogenol C hydrochloride
中文别名	2-[[2-[(4-甲氧基苯基)氨基]-4-嘧啶基]氨基]乙醇盐酸盐;4-溴吡啶-2,6-二甲酰胺
英文名称	Cardiogenol C hydrochloride
英文别名	Cardiogenol C, Hydrochloride;2-({2-[(4-Methoxyphenyl)amino]-4-pyrimidinyl}amino)ethanol hydroc hloride (1:1);Combretastatin A4;2-[[2-[(4-Methoxyphenyl)aMino]-4-pyriMidinyl]aMino]ethanol Hydrochloride;4-(2-HYDROXYETHYLAMINO)-2-(4-METHOXYPHENYLAMINO)-PYRIMIDINE HYDROCHLORIDE;2-[[2-[(4-Methoxyphenyl)amino]-4-pyrimidinyl]amino]ethanol hydrochloride (1:1);Cardiogenol C hydrochloride;Cardiogenol C (hydrochloride);Cardiogenol C HCl;2-[[2-(4-methoxyanilino)pyrimidin-4-yl]amino]ethanol;hydrochloride;2-((2-((4-methoxyphenyl)amino)pyrimidin-4-yl)amino)ethan-1-ol hydrochloride;MLS006010775;C13H16N4O2.HCl;BCP26174;1663AH
Cas No.	1049741-55-0
分子式	C₁₃H₁₇ClN₄O₂
分子量	296.75
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Cardiogenol C hydrochloride is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC₅₀=100 nM). Cardiogenol C hydrochloride also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C hydrochloride is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.

性状

Solid

IC50 & Target[1][2]

EC50: 100 nM (differentiation of ESCs into cardiomyocytes)

体外研究(In Vitro)

Cardiogenol C hydrochloride (1 μM; 7 days) has a cardiomyogenic effect on P19 cells, it significantly increases atrial natriuretic factor (ANF, nppa) in P19 cells when it compares to untreated control cells.
Cardiogenol C hydrochloride (0.01-100 μM; 7 days) significantly increases ANF expression. In addition, another frequently used cardiac marker gene (NKX2-5) is also significantly increased by this small molecule in C2C12 cells.
Cardiogenol C hydrochloride (0.001-100 μM; 7 days) increases cardiac Nav1.5 sodium channel protein expression as dose-dependent manner in C2C12 cells.
Cardiogenol C hydrochloride (1 μM; 35 days) addition from day 0 significantly increases myocardial differentiation and results in a significantly increased percentage of CBs with beating cardiomyocytes. This small moleculepromotes the development of beating cardiomyocytes in cardiovascular progenitor cell-derived cardiac bodies.
Cardiogenol C hydrochloride (0.01-100 μM; 7 days) does not effect cell growth even at 10 μM. In addition, Cardiogenol C either solves in water or DMSO generates a similar effect. The highest concentration, 100 μM has significant cellular toxicity on C2C12 cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

Cell Line:	C2C12 cells
Concentration:	0.01 μM; 0.1 μM; 1 μM; 3 μM; 10 μM; 30 μM; 100 μM
Incubation Time:	7 days
Result:	Increased ANF and NKX2.5 mRNA level as a dose-dependent manner.

Western Blot Analysis

Cell Line:	C2C12 cells
Concentration:	0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM
Incubation Time:	7 days
Result:	Increased cardiac Nav1.5 sodium channel protein levels.

Cell Proliferation Assay

Cell Line:	C2C12 cells
Concentration:	0.01 μM; 0.1 μM; 1 μM
Incubation Time:	7 days
Result:	Did not exert toxic effects on C2C12 cells at 0.01-10 μM treatment.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Wu X, et al. Small molecules that induce cardiomyogenesis in embryonic stem cells.J Am Chem Soc. 2004 Feb 18;126(6):1590-1. [Information]

[2]. Mike AK, et al. Small molecule cardiogenol C upregulates cardiac markers and induces cardiac functional properties in lineage-committed progenitor cells. Cell Physiol Biochem. 2014;33(1):205-21. [Information]

溶解度数据

体外研究:

DMSO : ≥ 59 mg/mL (198.82 mM)

H₂O : 2 mg/mL (6.74 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3698 mL	16.8492 mL	33.6984 mL
5 mM	0.6740 mL	3.3698 mL	6.7397 mL
10 mM	0.3370 mL	1.6849 mL	3.3698 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： PBS
Solubility: 3.33 mg/mL (11.22 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (8.42 mM); Clear solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.42 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.42 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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