ONO-7300243

SKU: orb1220433

Description

ONO-7300243 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; IC50 : 0.16 μM).

Key Properties

• CAS Number: 638132-34-0
• MW: 461.55
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₁NO₅
• SMILES: COc1cc(cc(OC)c1C)C(=O)N(CCCc1ccccc1)Cc1ccc(CC(O)=O)cc1
• Target: LPA Receptor
• Solubility: DMSO:100 mg/mL (216.66 mM)

Bioactivity

• 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).
  Read more...
• In Vitro:
  ONO-7300243 shows modest in vitro activity (IC50 = 0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

LPA Receptor