1. GPCR/G Protein
  2. LPL Receptor
  3. LPA1 antagonist 1

LPA1 antagonist 1 

Cat. No.: HY-18076
Handling Instructions

LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.

For research use only. We do not sell to patients.

LPA1 antagonist 1 Chemical Structure

LPA1 antagonist 1 Chemical Structure

CAS No. : 1396006-71-5

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LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.

IC50 & Target

IC50: 25 nM (LPA1)[1].

In Vitro

LPA1 antagonist 1 (compound 2) displays very potent and highly selective inhibitory activity toward LPA1, with little inhibition on LPA3 even at very high concentrations. To our knowledge, LPA1 antagonist 1 is the most selective nonlipid LPA1 antagonist so far reported. It appears that compounds (e.g., LPA1 antagonist 1) from the N-aryltriazole chemical class are much more selective for LPA1 than compounds from the corresponding pyrazole series. In comparison with Ki16425 and AM095, LPA1 antagonist 1 shows much improved antiproliferative activity. LPA1 antagonist 1 demonstrates the highest LPA1 selectivity and attenuated LPA-induced NHLF proliferation and contraction with high potency[1].

In Vivo

Oral dosing of LPA1 antagonist 1 in mice causes a dose-dependent reduction in serum histamine levels induced following intravenous LPA stimulation. When mice are orally dosed with LPA1 antagonist 1 (100 mg/kg, aqueous suspension) prior to intravenous LPA injection, the LPA-induced histamine level is significantly blocked A clear PK/PD relationship is demonstrated by the correlation between the levels of LPA1 antagonist 1 and LPA-induced histamine concentrations in plasma. Although AM095 almost completely blocks histamine release (100 mg/kg), analysis of plasma samples revealed more than 65-fold higher concentrations of AM095 than LPA1 antagonist 1 (100 mg/kg). The ability of LPA1 antagonist 1 to block histamine release at much lower plasma concentration suggests that further improvement of pharmacokinetic properties of this chemical class could lower the effective dose[1].

Molecular Weight







CC(N=N1)=C(NC(O[[email protected]@H](C2=CC=CC=C2)C)=O)N1C3=CC=C(C4=CC=C(C5(CC5)C(O)=O)C=C4)C=C3


Room temperature in continental US; may vary elsewhere.


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