chroman 1
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:作用于ROCK-II,IC50<1 nM。
Chroman 1是一种高度有效的ROCK-II抑制剂。ROCK是丝氨酸/苏氨酸激酶的AGC激酶家族的成员之一,由ROCK-I和ROCK-II两个高度同源的亚型组成。作为RhoA蛋白的下游效应物之一,ROCK通过肌球蛋白轻链磷酸化调节张力纤维的形成和肌动蛋白细胞骨架组构。目前,抑制Rho激酶(ROCK)来治疗各种疾病引起广泛关注。
体外:Chroman 1是一种亚纳摩尔的ROCK-II抑制剂,相比初步评估的相关激酶,如AKT1、蛋白激酶A(PKA)以及高度同源的Cdc42结合激酶,Chroman 1对ROCK-II具有中等至优良的选择性。另外,在基于功能细胞的肌球蛋白轻链双磷酸化试验中,Chroman 1也显示良好的体外活性[1]。
体内:大鼠药代动力学评价结果表明,Chroman 1相比其先导化合物苯并二恶烷和chroman可适度提高口服生物利用度(27-35%)。另外,Chroman 1还显示出独特又吸引人的药代动力学特性,通过口服递送可全身暴露[1]。
临床试验:目前尚无临床研究报道。
参考文献:
[1] Chen YT,Bannister TD,Weiser A,Griffin E,Lin L,Ruiz C,Cameron MD,Schürer S,Duckett D,Schrter T,LoGrasso P,Feng Y. Chroman-3-amides as potent Rho kinase inhibitors. Bioorg Med Chem Lett.2008 Dec 15;18(24):6406-9.
Storage | Store at -20°C |
M.Wt | 436.5 |
Cas No. | 1273579-40-0 |
Formula | C24H28N4O4 |
Synonyms | ROCK-II inhibitor |
Solubility | ≥50.3 mg/mL in DMSO; ≥3.81 mg/mL in EtOH with ultrasonic; insoluble in H2O |
Chemical Name | (3S)-N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-6-methoxy-3,4-dihydro-2H-chromene-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN(C)CCOC1=C(C=CC(=C1)C2=CNN=C2)NC(=O)C3CC4=C(C=CC(=C4)OC)OC3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
![chroman 1](http://www.apexbt.com/media/diy/images/struct/A3310.png)
相关生物数据
![chroman 1 chroman 1](http://www.apexbt.com/media/diy/images/wb/A3310_1.jpg)