LX7101 HCL
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 对LIMK2\KIMK1\ROCK1和ROCK2的IC50分别为4.3\32\69和32 nM.
LIM激酶1和2(LIMK1和LIMK2)通过磷酸化和去激活丝切蛋白(cofilin) 调节细胞骨架动力学,cofilin是解聚肌动蛋白微丝的一种蛋白.ROCK是LIMK信号级联的上游激酶,调节肌动蛋白丝动力学,在临床上研究发现其通过小梁网的松弛减少眼压.LX7101是LIM激酶和ROCK的双重抑制剂,用于治疗青光眼.
体外实验:LX7101对LIMK2具有显著更高的选择性.此外,针对403种激酶筛选出LX7101,在筛选中观察到适度的选择性,包括LIMK2和ROCK2在内的34个实验表明Kd值小于1 μM[1].
在体实验:与0.1％的制剂相比,在良好的耐受剂量下,LX7101实现眼压的额外减少,作用时间长,服用后超过8小时眼压才回到基线.更关键的是,与噻吗洛尔或拉坦前列素相比,LX7101更显著的降低眼压[1].
临床试验:LX7101完成IND的研究,并在青光眼患者的1期临床试验中进行检测,表明其降低眼内压的效力[1].
参考文献：
[1] Harrison BA, Almstead ZY, Burgoon H, Gardyan M, Goodwin NC, Healy J, Liu Y, Mabon R, Marinelli B, Samala L, Zhang Y, Stouch TR, Whitlock NA, Gopinathan S, McKnight B, Wang S, Patel N, Wilson AG, Hamman BD, Rice DS, Rawlins DB. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma. ACS Med Chem Lett. 2014 Nov 24;6(1):84-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 487.98 |
| Cas No. | 1192189-69-7 |
| Formula | C23H30ClN7O3 |
| Solubility | insoluble in H2O; insoluble in EtOH; insoluble in DMSO |
| Chemical Name | InChI=1S/C23H29N7O3.ClH/c1-15-12-25-19-18(15)20(27-14-26-19)30-9-7-23(13-24,8-10-30)21(31)28-16-5-4-6-17(11-16)33-22(32)29(2)3;/h4-6,11-12,14H,7-10,13,24H2,1-3H3,(H,28,31)(H,25,26,27);1H |
| SDF | Download SDF |
| Canonical SMILES | CC1=CNC2=NC=NC(N3CCC(C(NC4=CC(OC(N(C)C)=O)=CC=C4)=O)(CN)CC3)=C21.Cl |
| 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。 |
化学结构
