ONO-7300243
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为160 nM。
ONO-7300243是一种LPA1拮抗剂。
溶血磷脂酸(LPA)是一种生物活性类磷脂,由血液中自分泌运动因子从溶血磷脂酰胆碱产生。LPA具有广泛的细胞反应,例如细胞增殖、细胞内Ca2+动员、细胞存活和细胞运动性。基于其特定性质,LPA参与多种复杂的生理反应,例如平滑肌的收缩、伤口愈合、凝血、脱髓鞘以及免疫能力。
体外:经鉴定,ONO-7300243是一种新的和强效的LPA1拮抗剂。重要的是,研究发现ONO-7300243显示出与临床上用于治疗伴有良性前列腺增生(BPH)的排尿困难的α1肾上腺素受体拮抗剂坦索罗辛相当的效力[1]。
体内:动物研究报道,虽然ONO-7300243仅显示适度的体外活性(IC 50 =0.16 μM),但ONO-7300243对大鼠的口服给药对减少尿道内压力产生更强的作用(10 mg/kg i.d.时88%抑制,3 mg/kg i.d.时62%抑制)。与坦索罗辛相比,该剂量ONO-7300243对平均血压没有影响,这表明LPA1拮抗剂可用于治疗BPH而不影响血压[1]。
临床试验:到目前为止,ONO-7300243仍处于临床前研究阶段。
参考文献:
[1] Terakado M et al. Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead. ACS Med Chem Lett.2016 Aug 19;7(10):913-918. eCollection 2016.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 461.22 |
Cas No. | 638132-34-0 |
Formula | C28H31NO5 |
Solubility | ≥46.1 mg/mL in DMSO; insoluble in H2O; ≥11.55 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-(4-((3,5-dimethoxy-4-methyl-N-(3-phenylpropyl)benzamido)methyl)phenyl)acetic acid |
SDF | Download SDF |
Canonical SMILES | O=C(O)CC1=CC=C(CN(C(C2=CC(OC)=C(C)C(OC)=C2)=O)CCCC3=CC=CC=C3)C=C1 |
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
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