SBC-115076
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:N/A
PCSK9是一种丝氨酸蛋白酶,主要表达于肝脏与肠道中.PCSK9通过降低肝细胞中LDLR数量以发挥作用.PCSK9酶活性使其于胞内成熟并分泌.循环PCSK9结合细胞表面的LDLR,与LDLR一起进入细胞.PCSK9还可以结合细胞内的LDLR.因此,由于PCSK9是一种主要的LDLR抑制剂,PCSK9已成为一个热门的新药靶点,有望用于治疗高胆固醇血症以及冠心病.SBC-115076是一种抗PCSK9化合物.
体外:SBC-115076可以剂量依赖性地促进DHLDL摄取,但其效果较SBC-110034弱.此外,1.6 μM SBC-115076可以将细胞内LDLR水平提升数倍[1].
体内:在饲喂高脂肪饮食的小鼠中,SBC-115076降低胆固醇水平.结果表明,相对于高脂肪饮食的动物水平,SBC-115076于给药两周后使总胆固醇水平平均降低了32%,最终使总胆固醇水平平均减少了50%并恢复至正常饮食的胆固醇水平[1].
临床试验:截至目前,SBC-115076仍处于临床前开发阶段.
参考文献：
[1] Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases. Patent: WO 2014150326 A1
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 527.61 |
| Cas No. | 489415-96-5 |
| Formula | C31H33N3O5 |
| Solubility | ≥52.8 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 4-(4-(benzyloxy)-3-methylbenzoyl)-3-hydroxy-1-(3-morpholinopropyl)-5-(pyridin-4-yl)-1H-pyrrol-2(5H)-one |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(C(C(C(N2CCCN3CCOCC3)C4=CC=NC=C4)=C(O)C2=O)=O)=CC=C1OCC5=CC=CC=C5 |
| 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
