ONO-7300243

Catalog No.S8345 Synonyms: ONO 7300243, ONO7300243

ONO-7300243 Chemical Structure

Molecular Weight(MW): 461.55

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

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Biological Activity

Description ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
Targets
LPA1 [1]
(Cell-free assay)
0.16 μM
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].

Protocol

Cell Research:

[1]

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  • Cell lines: Chinese hamster ovary (CHO) cells
  • Concentrations: --
  • Incubation Time: --
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Rats
  • Formulation: 0.5% methyl cellulose
  • Dosages: 3 mg/kg for i.v. or 10 mg/kg for p.o.
  • Administration: i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.32 mM)
Ethanol 46 mg/mL (99.66 mM)
Water 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.

Chemical Information

Molecular Weight 461.55
Formula

C28H31NO5

CAS No. 638132-34-0
Storage powder
in solvent
Synonyms ONO 7300243, ONO7300243

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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LPA Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID