[CAS NO. 638132-34-0] ONO-7300243
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PRODUCTS SPECIFICATIONS [638132-34-0]
Catalog
SLK-S8345
Brand
Selleck
CAS
638132-34-0
DESCRIPTION [638132-34-0]
Overview
| MDL | MFCD30534399 |
|---|---|
| Molecular Weight | 461.55 |
| Molecular Formula | C28H31NO5 |
| SMILES | O=C(O)CC1=CC=C(CN(CCCC2=CC=CC=C2)C(C3=CC(OC)=C(C)C(OC)=C3)=O)C=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
ONO-7300243 is a novel, potent antagonist with an IC50 of 160 nM.
Targets
| LPA1 [1] (Cell-free assay) |
| 0.16 μM |
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).
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