638132-34-0
ONO-7300243
CAS: 638132-34-0
Molecular Formula: C28H31NO5
638132-34-0 - Names and Identifiers
| Name | ONO-7300243 |
| Synonyms | ONO-7300243 Benzeneacetic acid, 4-[[(3,5-dimethoxy-4-methylbenzoyl)(3-phenylpropyl)amino]methyl]- |
| CAS | 638132-34-0 |
638132-34-0 - Physico-chemical Properties
| Molecular Formula | C28H31NO5 |
| Molar Mass | 461.55 |
| Density | 1.180±0.06 g/cm3(Predicted) |
| Boling Point | 688.1±55.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 4.30±0.10(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | ONO-7300243 shows modest in vitro activity (IC 50 =0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro. |
| In vivo study | 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 (ID 50 =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). |
638132-34-0 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.167 ml | 10.833 ml | 21.666 ml |
| 5 mM | 0.433 ml | 2.167 ml | 4.333 ml |
| 10 mM | 0.217 ml | 1.083 ml | 2.167 ml |
| 5 mM | 0.043 ml | 0.217 ml | 0.433 ml |
Last Update：2024-01-02 23:10:35
638132-34-0 - Reference Information
| biological activity | ONO-7300243 is a novel potent antagonist of Lysophosphatidic acid receptor 1 (LPA1), the IC50 was 0.16 μm. |
| Target | IC50: 0.19-0.13 μm (LPA1) |
Last Update：2024-04-10 22:29:15
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