ONO-7300243

Catalog No.S8345 Batch:S834502

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Technical Data

Formula

C28H31NO5

Molecular Weight 461.55 CAS No. 638132-34-0
Solubility (25°C)* In vitro DMSO 92 mg/mL (199.32 mM)
Ethanol 46 mg/mL (99.66 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Cell Assay:

[1]

  • 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.

Animal Study:

[1]

  • Animal Models

    Rats

  • Dosages

    3 mg/kg for i.v. or 10 mg/kg for p.o.

  • Administration

    i.v. or p.o.

Selleck's ONO-7300243 has been cited by 1 publication

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.