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ONO-7300243

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Chemical Structure| 638132-34-0 同义名 : -
CAS号 : 638132-34-0
货号 : A254917
分子式 : C28H31NO5
纯度 : 98%
分子量 : 461.55
MDL号 : MFCD30534399
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
靶点

  • LPA1

    LPA1, IC50:0.16 μM
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].
实验方案
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
参考文献

[1]Terakado M, Suzuki H, 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 Oct 13.