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CAS No.: 638132-34-0

ONO-7300243 Catalog No. CSN18971

Synonyms: ONO-7300243

ONO-7300243 is a potent LPA1 (Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.

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生物活性

实验方案

技术信息

生物活性

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].

动物研究

剂量

Rat^[1] (p.o.): 10 mg/kg, 30 mg/kg

给药途径

p.o.

动物药代数据

Animal	Rats^[1]
Dose	3 mg/kg (i.v.) 10 mg/kg (p.o.)
Administration	i.v. p.o.
C_max	343 ± 204 ng/ml (p.o.)
T_1/2	0.3 ± 0 h (i.v.) 1.8 ± 1.7 h (p.o.)
F	7.3% (p.o.)
T_max	1.3 ± 0.6 h (p.o.)
AUC	3286 ± 215 ng･h/ml (i.v.) 800 ± 413 ng･h/ml (p.o.)
Vss	223 ± 42 ml/kg (i.v.)
CL_tot	15.9 ± 1.0 ml/min/kg

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1666 mL
- 10.8331 mL
- 21.6661 mL
- 5 mM
- 0.4333 mL
- 2.1666 mL
- 4.3332 mL
- 10 mM
- 0.2167 mL
- 1.0833 mL
- 2.1666 mL

技术信息

CAS号

638132-34-0

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H31NO5

运输

蓝冰

分子量

461.55

别名

ONO-7300243

溶解度

DMSO	200.0 mg/mL (433.3 mM)
Water	insoluble

动物实验配方

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