ONO-7300243

製品コードS8345 バッチS834501

印刷

化学情報

Chemical Structure Synonyms ONO 7300243, ONO7300243 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H31NO5
分子量 461.55 CAS No. 638132-34-0
Solubility (25°C)* 体外 DMSO 92 mg/mL (199.32 mM)
Ethanol 92 mg/mL (199.32 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
in vitro Although ONO-7300243 showed only modest in vitro activity (IC50 = 0.16 μM), it showed much stronger effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.). ONO-7300243 showed good membrane permeability and good metabolic stability against rat liver microsomes[1].
in vivo ONO-7300243 inhibited the LPA-induced IUP(intraurethral pressure) 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 (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). In a a rat pharmacokinetic study, ONO-7300243 showed a rapid clearance (CLtot = 15.9 mL/min/kg at 3 mg/kg i.v.) and a short half-life (0.3 h)[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Chinese hamster ovary (CHO) cells
濃度 --
反応時間 --
実験の流れ

Chinese hamster ovary (CHO) cells stably expressing human LPA1 were seeded at a density of 2×104 cells per well into 96-well plates and cultured in the culture medium (F-12 Nutrient Mixture (HAM) containing 10% FBS) in a CO2 incubator (37ºC, 5% CO2, 95% air) for 2 days. Load buffer (culture medium containing 5 µM Fura2-AM, 10 mM HEPES (pH 7.55) and 2.5 mM probenecid) was added in each well and incubated in the CO2 incubator for 1 hour. After the load buffer was removed, cells were rinsed with assay buffer at room temperature, and the assay buffer was added to the cells. In the experiment of LPA1 antagonist assay, intracellular Ca2+ concentration was monitored using a fluorescence drug screening system to measure the ratio of fluorescence intensities (f340/f380) at 500 nm. After pretreatment of the antagonists, lysophosphatidic acid (LPA, final 100 nM) was added to the cells. The inhibition rate (%) of the antagonists was calculated from the peak ratio of LPA after treatment of compounds and that of control (DMSO). Furthermore, a non-linear regression analysis was performed using the Sigmoid Emax Model to estimate IC50 values.
動物実験 動物モデル Rats
投薬量 3 mg/kg for i.v. or 10 mg/kg for p.o.
投与方法 i.v. or p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

LPA receptor1 antagonists as anticancer agents suppress human lung tumours. [ Eur J Pharmacol, 2020, 868:172886] PubMed: 31866407

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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