| CAS NO: | 638132-34-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 461.55 |
|---|---|
| Formula | C28H31NO5 |
| CAS No. | 638132-34-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 92 mg/mL (199.3 mM) |
| Water: <1 mg/mL | |
| Ethanol: 92 mg/mL (199.3 mM) | |
| SMILES Code | O=C(O)CC1=CC=C(CN(C(C2=CC(OC)=C(C)C(OC)=C2)=O)CCCC3=CC=CC=C3)C=C1 |
| Synonyms | ONO 7300243, ONO7300243; ONO-7300243 |
| In Vitro | In vitro activity: ONO-7300243 (also named as ONO 7300243, ONO7300243) is a novel, potent and selective antagonist of LPA1(Lysophosphatidic Acid Receptor) with an IC50 of 160 nM. ONO-7300243 was identified from a high throughout screening and subsequent structural optimizaiton. A Kinase Assay: ONO-7300243 shows modest in vitro activity (IC50=0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro. Cell Assay: lthough 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. |
|---|---|
| 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). |
| Animal model | Rats |
| Formulation & Dosage | Formulated in 0.5% methyl cellulose; 3 mg/kg for i.v. or 10 mg/kg for p.o.; i.v. or p.o. |
| References | ACS Med Chem Lett. 2016 Aug 19;7(10):913-918. |
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