1. GPCR/G Protein
  2. LPL Receptor

ONO-7300243 

Cat. No.: HY-100882 Purity: 98.04%
Data Sheet SDS Handling Instructions

ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.

For research use only. We do not sell to patients.
ONO-7300243 Chemical Structure

ONO-7300243 Chemical Structure

CAS No. : 638132-34-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 145 In-stock
5 mg USD 132 In-stock
10 mg USD 228 In-stock
25 mg USD 480 In-stock
50 mg USD 864 In-stock
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200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.

IC50 & Target

IC50: 0.19-0.13 μM (LPA1)[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].

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1666 mL 10.8331 mL 21.6661 mL
5 mM 0.4333 mL 2.1666 mL 4.3332 mL
10 mM 0.2167 mL 1.0833 mL 2.1666 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

ONO-7300243 is prepared in 0.5% methylcellulose[1].

Rats[1]
The oral administration of ONO-7300243 (30 mg/kg, p.o.) is investigated to determine its effect on rat IUP. ONO-7300243 is studied in an LPA-induced rat intraurethral pressure (IUP) model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

461.55

Formula

C₂₈H₃₁NO₅

CAS No.

638132-34-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ONO-7300243
Cat. No.:
HY-100882
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