Home GPCR & G Protein LPA Receptor antagonist ONO-7300243 For research use only.

ONO-7300243

Synonyms: ONO 7300243, ONO7300243

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

ONO-7300243 Chemical Structure

ONO-7300243 Chemical Structure

CAS No. 638132-34-0

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ONO-7300243 Related Products

Signaling Pathway

LPA Receptor Signaling Pathways

LPA Receptor Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Rats
Dosages 3 mg/kg for i.v. or 10 mg/kg for p.o.
Administration i.v. or p.o.

Chemical Information & Solubility

Molecular Weight 461.55 Formula

C28H31NO5
CAS No. 638132-34-0 SDF Download ONO-7300243 SDF
Smiles CC1=C(C=C(C=C1OC)C(=O)N(CCCC2=CC=CC=C2)CC3=CC=C(C=C3)CC(=O)O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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