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ONO-7300243

  Cat. No.:  DC10630   Featured
Chemical Structure
638132-34-0
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More than 5000 active chemicals with high quality for research!
Field of application
ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 638132-34-0
SMILES: O=C(O)CC1=CC=C(CN(C(C2=CC(OC)=C(C)C(OC)=C2)=O)CCCC3=CC=CC=C3)C=C1
Formula: C28H31NO5
M.Wt: 461.55
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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