ONO-7300243
产品编号: DC10630
我们的合作伙伴:
中国地区超过5000个高品质化合物库存
应用领域
ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
| Cas No.: |
638132-34-0 |
| 名称: |
|
| 别名: |
|
| SMILES: |
O=C(O)CC1=CC=C(CN(C(C2=CC(OC)=C(C)C(OC)=C2)=O)CCCC3=CC=CC=C3)C=C1 |
| 分子式: |
C28H31NO5 |
| 分子量: |
461.55 |
| 纯度: |
|
| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
|
| In Vivo: |
|
| In Vitro: |
|
| References: |
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.
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). |
| Kinase Assay: |
|
| Cell Assay: |
|
| Animal Administration: |
|
| References: |
|
MSDS
COA
| LOT NO. |
DOWNLOAD |
|
|
| 2018-0101 |
|
询盘
