ONO-7300243

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

Inhibitor|Lysophospholipid Receptor|LPA Receptor|LPL|LPA1|LPAReceptor|LPLReceptor|LPL Receptor|ONO 7300243|ONO7300243|ONO-7300243|inhibit



产品信息

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|G 蛋白偶联受体
分子量 461.55
纯度 99.66%, 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 | Shipping with blue ice.
别名 Inhibitor|Lysophospholipid Receptor|LPA Receptor|LPL|LPA1|LPAReceptor|LPLReceptor|LPL Receptor|ONO 7300243|ONO7300243|ONO-7300243|inhibit

靶点活性

LPA1:0.19-0.13 μM (IC50)

体内活性

通过口服给药ONO-7300243 来确定其对大鼠IUP的影响。ONO-7300243 以剂量依赖性方式抑制了LPA诱导的IUP增加(ID50 = 11.6 mg/kg p.o.),直到给药后1小时。在10和30mg/kg剂量下观察到显着效果(p < 0.05 vs vehicle). ONO-7300243 (30 mg/kg, p.o.)在没有LPA刺激的情况下,与vehicle比较,显着降低了清醒大鼠的IUP,同时不影响平均血压(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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