638132-34-0
638132-34-0 structure
- Name: ONO-7300243
- Chemical Name: ONO-7300243
- CAS Number: 638132-34-0
- Molecular Formula: C28H31NO5
- Molecular Weight: 461.549
- Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
- Create Date: 2018-05-11 10:49:19
- Modify Date: 2024-01-31 10:13:01
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ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
| Name | ONO-7300243 |
|---|---|
| Synonyms |
Benzeneacetic acid, 4-[[(3,5-dimethoxy-4-methylbenzoyl)(3-phenylpropyl)amino]methyl]-
(4-{[(3,5-Dimethoxy-4-methylbenzoyl)(3-phenylpropyl)amino]methyl}phenyl)acetic acid |
| Description | ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.19-0.13 μM (LPA1)[1] |
| In Vitro | ONO-7300243 shows modest in vitro activity (IC50=0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro[1]. |
| In Vivo | ONO-7300243 shows good efficacy in vivo. The oral dosing of 17a at 30 mg/kg leads to reduced intraurethral pressure in rats. ONO-7300243 shows stronge effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.) compared with compound 12g. The results reveal that ONO-7300243 shows good membrane permeability and good metabolic stability against rat liver microsomes (MS). ONO-7300243 exhibits good selectivity towards LPAl over LPA2, most likely because low molecular weight and low lipophilicity lead to reduced compound promiscuity and increased selectivity. ONO-7300243 inhibits the LPA-induced IUP increase in a dose dependent manner (ID50=11.6 mg/kg p.o.) up to 1 h after dosing. Significant effects are observed at 10 and 30 mg/kg (p<0.05 vs.vehicle). ONO-7300243 (30 mg/kg, p.o.) leads to a significant decrease in the IUP in conscious rats without LPA stimulation compared with the vehicle without affecting the mean blood pressure (MBP). The results of a rat pharmacokinetic study of ONO-7300243 show that this material had 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 Admin | Rats[1] The oral administration of ONO-7300243 (30 mg/kg, p.o.) is investigated to determine its effect on rat IUP. ONO-7300243 is studied in an LPA-induced rat intraurethral pressure (IUP) model. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 688.1±55.0 °C at 760 mmHg |
| Molecular Formula | C28H31NO5 |
| Molecular Weight | 461.549 |
| Flash Point | 369.9±31.5 °C |
| Exact Mass | 461.220215 |
| LogP | 5.59 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.591 |
| Storage condition | -20℃ |