ONO-7300243 is a potent LPA1 (Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
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描述 | LPA (lysophosphatidic acid), which has been shown to be involved in certain diseases such as atherosclerosis and cancer, can act through its receptor like LPA receptor 1, LPA receptor 2, or LPA receptor 3 and elicit different biological actions, like Ca2+ mobilization, changing in cAMP accumulation, changing cell shape and motility, and cell proliferation. ONO-7300243 is a potent and selective LPA1 receptors antagonist with IC50 value of 0.16μM (measured by intracellular Ca2+ concentration), much more potent to LPA2 receptor (IC50=8.6μM) and LPA3 receptor (IC50>10μM). ONO-7300243 could inhibit LPA-induced [Ca22+] increase. ONO-7300243 showed strong effects on benign prostatic hyperplasia (BPH). Oral administration of ONO-7300243 at dose of 30mg/kg led to reduced intraurethral pressure in rats. |
作用机制 | The basic residues in the active site of of LPA1 can form interactions with acidic functional groups of ONO-7300243[1]. |
Dose | Rat[1] (p.o.): 10 mg/kg, 30 mg/kg | ||||||||||||||||||||
Administration | p.o. | ||||||||||||||||||||
Pharmacokinetics |
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计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.83mL 2.17mL 1.08mL |
21.67mL 4.33mL 2.17mL |
CAS号 | 638132-34-0 |
分子式 | C28H31NO5 |
分子量 | 461.55 |
SMILES Code | O=C(O)CC1=CC=C(CN(CCCC2=CC=CC=C2)C(C3=CC(OC)=C(C)C(OC)=C3)=O)C=C1 |
MDL No. | MFCD30534399 |
别名 | |
运输 | 蓝冰 |
InChI Key | WGABOZPQOOZAOI-UHFFFAOYSA-N |
Pubchem ID | 66775043 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, store in freezer, under -20°C |
溶解方案 |
DMSO: 105 mg/mL(227.49 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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