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ONO-7300243

ONO-7300243 是溶血磷脂酸受体 1 (LPA1)拮抗剂，IC50为 0.16 μM。

CAS号

638132-34-0

分子式

C28H31NO5

主要靶点

LPA Receptor|LPL Receptor

仅限科研使用

Cat No : CM04985

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Synonyms

验证数据展示

  • CAS No.: 638132-34-0

    ONO-7300243
    CAS#: 638132-34-0

产品信息

ONO-7300243 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; IC50 : 0.16 μM).

CAS号 638132-34-0
分子式 C28H31NO5
主要靶点 LPA Receptor|LPL Receptor
主要通路 G蛋白偶联受体
分子量 461.55
纯度 ， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

LPA1:0.19-0.13 μM (IC50)

体内活性

The oral administration of ONO-7300243 (17a) to determine its effect on rat IUP. Compound 17a inhibited the LPA-induced IUP increase in a dose-dependent manner (ID50 = 11.6 mg/kg p.o.) up to 1 h after dosing. Significant effects were observed at 10 and 30 mg/kg (p < 0.05 vs vehicle). ONO-7300243 (17a) (30 mg/kg, p.o.) led to a significant decrease in the IUP in conscious rats without LPA stimulation compared with the vehicle without affecting the mean blood pressure (MBP)[1].

溶解度

DMSO:100 mg/mL (216.66 mM)

参考文献

1.Terakado M , Suzuki H , Hashimura K , et al. Discovery of ONO-7300243 from a novel class of Lysophosphatidic Acid Receptor 1 antagonists: From hit to lead.[J]. ACS Medicinal Chemistry Letters, 2016:acsmedchemlett.6b00225.
2.Terakado M , Suzuki H , Hashimura K , et al. Discovery of a Slow Tight Binding LPA1 Antagonist (ONO-0300302) for the Treatment of Benign Prostatic Hyperplasia[J]. ACS Medicinal Chemistry Letters, 2017:acsmedchemlett.7b00383.

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